Search Result
Results for "
opioid receptors agonist
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-107743
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NalBzoH
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Opioid Receptor
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Neurological Disease
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Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect .
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- HY-105604
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- HY-136623
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- HY-163667
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Opioid Receptor
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Neurological Disease
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Atoxifent is a potent μ-opioid receptor agonist (EC50=0.39 nM). These receptors are found in brain regions that control pain, emotions, habitual learning, and cognition. Atoxifent exhibits strong analgesic effects and a lower risk of respiratory depression. Atoxifent can be used for research in opioid pharmacology and signal transduction .
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- HY-147560
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Sigma Receptor
Opioid Receptor
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Neurological Disease
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σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .
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-
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- HY-P10395
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-
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- HY-162771
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor agonist 1 (compound 12) is a Mu opioid receptor agonist. Mu opioid receptor agonist 1 can be used in nervous system related research .
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-
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- HY-P10203
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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- HY-155319
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Opioid Receptor
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Neurological Disease
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μ opioid receptor agonist 3 (compound 20) is a potent μ opioid receptor (µOR) agonist with an EC50 of 0.87 nM. μ opioid receptor agonist 3 has the potential for pain and neuropsychiatric indications research .
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- HY-160761
-
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Opioid Receptor
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Inflammation/Immunology
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K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .
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- HY-P1481
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-
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- HY-19467
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-
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- HY-123689A
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ALKS-33 hydrochloride; RDC-0313 hydrochloride
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Opioid Receptor
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Neurological Disease
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Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo .
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- HY-P1087
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Metorphamide
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Opioid Receptor
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Cancer
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Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
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- HY-123689
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ALKS-33; RDC-0313
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Opioid Receptor
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Neurological Disease
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Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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-
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- HY-P1467
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-
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- HY-P1467A
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5-Methionine-enkephalin amide TFA
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Opioid Receptor
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Neurological Disease
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[Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ ζ opioid receptors.
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- HY-P1334
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-
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- HY-P3376
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-
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- HY-P1334A
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-
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- HY-123689S
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ALKS-33-d4; RDC-0313-d4
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Isotope-Labeled Compounds
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Neurological Disease
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-123689S1
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ALKS-33-d5; RDC-0313-d5
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Isotope-Labeled Compounds
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Neurological Disease
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Samidorphan-d5 (ALKS-33-d5) is a tritiated version of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
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- HY-P1502
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Opioid Receptor
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Neurological Disease
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β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
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- HY-13101
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- HY-P1013
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- HY-P1333
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
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- HY-121800
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- HY-151811
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Opioid Receptor
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Neurological Disease
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NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
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- HY-P10006
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Opioid Receptor
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Neurological Disease
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Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
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- HY-P1333A
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
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- HY-120456
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Opioid Receptor
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Neurological Disease
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SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect .
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- HY-P1470
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- HY-P1336
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- HY-P1337
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- HY-P1013A
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- HY-P3445
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- HY-P3445A
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- HY-P1481A
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- HY-156131
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ADL 2-1294
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Opioid Receptor
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Inflammation/Immunology
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Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent .
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- HY-P1337A
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- HY-145369
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- HY-138984
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- HY-101039A
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Opioid Receptor
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Neurological Disease
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AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
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- HY-101039
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- HY-P0088
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Dynorphin A Porcine Fragment 1-13
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Opioid Receptor
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Others
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Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
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- HY-111454
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- HY-101386
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- HY-136586
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- HY-121415
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- HY-107747
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- HY-156972
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Opioid Receptor
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Metabolic Disease
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NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats .
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- HY-122681
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Opioid Receptor
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Neurological Disease
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SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioid receptor partial agonist, with high binding affinity (NOP receptor Ki=7.49; μ-Opioid receptor Ki=2.70). SR-16435 can relieve pain .
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- HY-153471
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- HY-P1577
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- HY-B0418AS
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- HY-14157
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Opioid Receptor
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Inflammation/Immunology
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ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms .
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- HY-14157A
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Opioid Receptor
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Inflammation/Immunology
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ADL-5747 hydrochloride is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 hydrochloride activates these receptors, thereby playing a role in pain management pathways. ADL-5747 hydrochloride can be used for research into pain management mechanisms .
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- HY-P0244
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- HY-107747A
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- HY-P2018
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- HY-P3517
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β-EP (6-31), human
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Opioid Receptor
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Neurological Disease
Endocrinology
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β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
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- HY-155707
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Others
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Inflammation/Immunology
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MOR agonist-3 (Compound 84) is a D3R/MOR antagonist (Ki 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioid receptor) (HY-149337) partial agonists and to reduce opioid abuse through D3R antagonists. MOR agonist-3 can be used in the treatment of inflammation and neuropathic pain research .
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- HY-142919
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Opioid Receptor
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Neurological Disease
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μ opioid receptor agonist 2 (Compound H-3)is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases .
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- HY-142918
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Opioid Receptor
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Neurological Disease
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μ opioid receptor agonist 1 (Compound H-1a)is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases .
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- HY-141468
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β-CNA dihydrochloride
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Opioid Receptor
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Neurological Disease
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β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception .
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- HY-P0210
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DAMGO
4 Publications Verification
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Opioid Receptor
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Cancer
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DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-P0244A
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- HY-P3555
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- HY-P3870
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Opioid Receptor
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Neurological Disease
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DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects .
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- HY-P3870A
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Opioid Receptor
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Neurological Disease
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DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
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- HY-19206
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- HY-B1052
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- HY-B1052A
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- HY-P10394
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- HY-19231
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Org 41793
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Opioid Receptor
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Neurological Disease
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DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .
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- HY-101317A
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SB-205607
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Opioid Receptor
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Metabolic Disease
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TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
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- HY-P3609
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JNJ 38488502; FE 200665
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Opioid Receptor
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Neurological Disease
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CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-10487
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- HY-P0210B
-
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Opioid Receptor
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Cancer
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DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-101205
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- HY-P3555A
-
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Opioid Receptor
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Others
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D-Ala-Gly-Phe-Met-NH2 monoacetate, an opioid peptide, is a potent opiate δ-receptor agonist .
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- HY-156988
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- HY-162552
-
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Opioid Receptor
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Neurological Disease
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KOR/DOR agonist 2 is a KOR and DOR opioid receptors agonist with Ki values of 0.14 nM, and 0.93 nM, respectively. KOR/DOR agonist 2 shows significant antinociceptive effects. KOR/DOR agonist 2 penetrates the blood-brain barrier .
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- HY-P1198
-
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
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- HY-P3870B
-
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Opioid Receptor
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Neurological Disease
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DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects .
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- HY-163017
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- HY-100963
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- HY-P3043
-
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Opioid Receptor
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Neurological Disease
|
Bilaid A is a μ-opioid receptor agonist that can be extracted from Penicillium. The Ki value is 3.1 μM. Bilaid A can be used in pain research .
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- HY-15536
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GRT6005
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Opioid Receptor
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Neurological Disease
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Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
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- HY-P1170
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Ac-L-Tyr-Gly-Gly-L-Phe-D-Leu-COOH
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Opioid Receptor
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Neurological Disease
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N-terminally acetylated Leu-enkephalin is the N-terminally acetylated form of Leu-enkephalin. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
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- HY-P1198A
-
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
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- HY-161812
-
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Opioid Receptor
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Others
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MOR agonist-4 (2d) is a G protein signaling-biased Kappa opioid receptor (KOR) agonist with an EC50 value of 11 nM. MOR agonist-4 contains an electron withdrawing CF3 group and a bias factor of 38 based on triazole. MOR agonist-4 is used in the research of pruritis and analgesia .
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- HY-121974
-
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Others
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Neurological Disease
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SR14150 is a partial agonist of the NOP receptor with high affinity. The biological activity of SR14150 makes it potentially useful for the development of a new generation of multi-target opioids designed to simultaneously improve analgesia and reduce side effects. The activity of SR14150 and its interaction with other opioid receptors may provide new inhibitory options for the management of chronic pain .
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- HY-P0288
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Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin
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Opioid Receptor
Endogenous Metabolite
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Neurological Disease
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[Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
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- HY-107722
-
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Opioid Receptor
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Neurological Disease
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SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect .
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- HY-15997B
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(±)-Trans-(1R,2R)-U-50488 hydrochloride
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Opioid Receptor
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Neurological Disease
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(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .
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- HY-15997C
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(±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride
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Opioid Receptor
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Neurological Disease
|
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .
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- HY-P1317
-
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Opioid Receptor
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Neurological Disease
|
Nociceptin (1-13), amide is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes .
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- HY-P1317A
-
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Opioid Receptor
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Neurological Disease
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Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes .
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- HY-P0186
-
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Opioid Receptor
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Neurological Disease
|
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
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- HY-145128
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-
- HY-107751
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-
- HY-105235
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CI-977
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Opioid Receptor
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Neurological Disease
|
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
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- HY-105235A
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CI-977 hydrochloride
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Opioid Receptor
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Neurological Disease
|
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
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- HY-P1332
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[D-Ser2, Leu5, Thr6]-enkephalin
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Opioid Receptor
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Neurological Disease
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DSLET ([D-Ser2, Leu5, Thr6]-enkephalin) is a highly specific agonist of the δ-receptor. DSLET is an enkephalin-related peptide selectively bound to the δ opioid receptor .
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- HY-162850
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-
- HY-B0418A
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R-18553 hydrochloride
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Opioid Receptor
Autophagy
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Neurological Disease
Metabolic Disease
Cancer
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Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
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- HY-P0288A
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-
- HY-163917
-
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Opioid Receptor
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Neurological Disease
|
SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .
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- HY-120511
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KNT-127
1 Publications Verification
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Opioid Receptor
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Neurological Disease
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KNT-127 is a potent and selective δ-opioid receptor agonist effective by systemic administration. KNT-127 shows selectivity for the δ-receptor (Ki 0f 21.3, 0.16, 153 nM for opioid μ-, δ-, and κ-receptors, respectively). KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens and median pre-frontal cortex. Antidepressant-like effects .
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- HY-P0186A
-
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Opioid Receptor
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Neurological Disease
|
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
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- HY-129271
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Deltorphin A; Dermenkephalin
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Opioid Receptor
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Others
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Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
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- HY-163916
-
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Opioid Receptor
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Neurological Disease
|
SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders .
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-
- HY-120949
-
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Opioid Receptor
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Neurological Disease
|
(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .
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- HY-105627A
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CI-572 hydrochloride
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GABA Receptor
iGluR
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Cardiovascular Disease
|
Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR .
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- HY-159088
-
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Opioid Receptor
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Neurological Disease
|
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
|
-
- HY-163065
-
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
|
-
- HY-G0021
-
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-101078A
-
CMI 545 dihydrochloride
|
Others
|
Neurological Disease
|
(±)-Epibatidine (CMI 545) dihydrochloride is an agonist of nicotinic with potent analgetic activity. (±)-Epibatidine (CMI 545) dihydrochloride is an alkaloid originally characterized from frog skin. (±)-Epibatidine (CMI 545) dihydrochloride have little or no activity at a variety of other central receptors, including opioid receptors, muscarinic receptors, adrenergic receptors, dopamine receptors, serotonin receptors, and gamma-aminobutyric acid receptors .
|
-
- HY-107741
-
|
Opioid Receptor
|
Neurological Disease
|
SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys .
|
-
- HY-G0021S
-
Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
|
-
- HY-G0021S1
-
Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
|
-
- HY-112692
-
|
Opioid Receptor
|
Neurological Disease
|
AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects .
|
-
- HY-112692A
-
|
Opioid Receptor
|
Neurological Disease
|
AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects .
|
-
- HY-117436
-
|
Dopamine Receptor
|
Cardiovascular Disease
|
R(+)-6-Bromo-APB hydrobromide is a dopamine (DA) agonist. R(+)-6-Bromo-APB hydrobromide increased the expression of µ opioid receptor (MOR) mRNA in the nucleus accumbens .
|
-
- HY-105236
-
(Rac)-CI-977 free base
|
Others
|
Neurological Disease
|
(Rac)-Enadoline ((Rac)-CI-977 free base) is a selective K-opioid receptor agonist that stereoselectively antagonizes clonic seizures induced by slow intravenous injection of N-methyl-DL-aspartate in mice .
|
-
- HY-123389
-
(R)-UM-1071
|
Opioid Receptor
|
Endocrinology
|
MR2034 ((R)-UM-1071) is a κ-opioid receptor agonist with activity that stimulates the hypothalamic-pituitary-adrenal axis. MR2034 has shown the potential to promote mood and inhibit addictive behaviors in animal models and can be used to study inhibitory approaches related to mood and addictive disorders. MR2034 is selective for κ-opioid receptors and can effectively modulate biological processes related to stress and mood .
|
-
- HY-P3647
-
-
- HY-P3647A
-
|
Opioid Receptor
Adenylate Cyclase
|
Neurological Disease
|
[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .
|
-
- HY-130176
-
|
Opioid Receptor
ERK
Adenylate Cyclase
|
Neurological Disease
|
UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
|
-
- HY-B1052S
-
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Lofexidine-d4 (hydrochloride) (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride. Lofexidine hydrochloride is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
|
-
- HY-P1316
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
|
-
- HY-P1316A
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
|
-
- HY-17609
-
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
|
-
- HY-P1338
-
|
Opioid Receptor
|
Neurological Disease
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
|
-
- HY-P4107
-
|
Opioid Receptor
|
Neurological Disease
|
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr) .
|
-
- HY-111011
-
JNJ 38488502 acetate; FE 200665 acetate
|
Others
|
Neurological Disease
|
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.
|
-
- HY-12363
-
|
Opioid Receptor
|
Neurological Disease
|
U-69593 is a potent and selective κ1-opioid receptor agonist . U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
|
-
- HY-128865
-
|
Opioid Receptor
|
Neurological Disease
|
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects .
|
-
- HY-106756
-
U-62066
|
Opioid Receptor
|
Neurological Disease
|
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-124959
-
U-62066 mesylate
|
Opioid Receptor
|
Neurological Disease
|
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
|
-
- HY-134189
-
|
Opioid Receptor
Sigma Receptor
|
Neurological Disease
|
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
|
-
- HY-P0185
-
|
Opioid Receptor
|
Neurological Disease
|
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
|
-
- HY-P1338A
-
|
Opioid Receptor
|
Neurological Disease
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
|
-
- HY-P0185A
-
|
Opioid Receptor
|
Neurological Disease
|
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
|
-
- HY-P4053
-
|
Opioid Receptor
|
Neurological Disease
|
Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity .
|
-
- HY-101079
-
|
Opioid Receptor
|
Neurological Disease
|
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .
|
-
- HY-B0418AR
-
R-18553 hydrochloride (Standard)
|
Opioid Receptor
Autophagy
|
Neurological Disease
Metabolic Disease
Cancer
|
Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist . Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect .
|
-
- HY-P3044
-
|
Opioid Receptor
|
Neurological Disease
|
Bilaid A1e (Compound 1e) is a tetrapeptide agonist of the µ-opioid receptor (Ki = 750 nM). Bilaid A1e can be isolated from an Australian estuarine isolate of Penicillium sp. Bilaid A1e can be used for pain research .
|
-
- HY-161539
-
|
Opioid Receptor
|
Neurological Disease
|
KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .
|
-
- HY-134189A
-
|
Sigma Receptor
Opioid Receptor
|
Neurological Disease
|
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
|
-
- HY-P3634
-
|
Opioid Receptor
|
Neurological Disease
|
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
|
-
- HY-129668
-
|
Adrenergic Receptor
|
Neurological Disease
|
Bremazocine is a potent opioid kappa receptor agonist with analgesic activity. Bremazocine induces peripheral analgesia by releasing endogenous norepinephrine. The analgesic effect of bremazocine is associated with interaction with adenosine receptors. Bremazocine produces a dose-dependent peripheral analgesia after topical application. The effect of bremazocine is affected by nonselective α(2) adrenaline receptor antagonists, suggesting that it acts through a norepinephrine pathway .
|
-
- HY-10233
-
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
|
-
- HY-101317
-
SB-205607 dihydrobromide
|
Opioid Receptor
|
Neurological Disease
|
TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke .
|
-
- HY-126910
-
|
Opioid Receptor
|
Metabolic Disease
|
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .
|
-
- HY-12844
-
|
Opioid Receptor
|
Neurological Disease
|
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .
|
-
- HY-P1301
-
|
Opioid Receptor
|
Neurological Disease
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
-
- HY-110302
-
|
Opioid Receptor
|
Neurological Disease
|
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
|
-
- HY-P1301A
-
|
Opioid Receptor
|
Neurological Disease
|
[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
|
-
- HY-P1626
-
|
Opioid Receptor
|
Neurological Disease
|
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
|
-
- HY-P4679
-
E2078
|
Opioid Receptor
|
Neurological Disease
|
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .
|
-
- HY-163277
-
|
Opioid Receptor
|
Inflammation/Immunology
|
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
|
-
- HY-14356
-
-
- HY-162728
-
|
Opioid Receptor
|
Neurological Disease
|
RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC50 value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .
|
-
- HY-130696
-
(+)-Trans-(1R,2R)-U-50488
|
Opioid Receptor
|
Neurological Disease
|
(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
|
-
- HY-15997A
-
(+)-Trans-(1R,2R)-U-50488 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
|
-
- HY-13044
-
-
- HY-P1300
-
|
Opioid Receptor
|
Neurological Disease
|
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
- HY-N0923
-
(+)-Corydaline; Corydalin
|
Cholinesterase (ChE)
Enterovirus
Opioid Receptor
|
Neurological Disease
|
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
|
-
- HY-11051
-
|
Opioid Receptor
|
Inflammation/Immunology
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
|
-
- HY-P1300A
-
|
Opioid Receptor
|
Neurological Disease
|
[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
|
-
- HY-15997
-
(-)-Trans-(1S,2S)-U-50488 hydrochloride
|
Opioid Receptor
|
Infection
Cancer
|
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM) .
|
-
- HY-120645
-
|
Opioid Receptor
|
Neurological Disease
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
|
-
- HY-N0164
-
Matrine
Maximum Cited Publications
12 Publications Verification
Matridin-15-one; Vegard; α-Matrine
|
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
|
-
- HY-101202A
-
(Rac)-NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
(Rac)-SNC80 is a racemate of SNC80 (HY-101202). SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
|
-
- HY-N0923R
-
|
Cholinesterase (ChE)
Enterovirus
Opioid Receptor
|
Neurological Disease
|
Corydaline (Standard) is the analytical standard of Corydaline. This product is intended for research and analytical applications. Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioid receptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
|
-
- HY-101202
-
NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment .
|
-
- HY-N0164R
-
|
PINK1/Parkin
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
Apoptosis
|
Inflammation/Immunology
Cancer
|
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
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- HY-120045A
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Opioid Receptor
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Neurological Disease
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DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1087
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Metorphamide
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Opioid Receptor
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Cancer
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Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
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- HY-P1467A
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5-Methionine-enkephalin amide TFA
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Opioid Receptor
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Neurological Disease
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[Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ ζ opioid receptors.
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- HY-P1334
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- HY-P1334A
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- HY-136623
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- HY-P10395
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- HY-P10203
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Opioid Receptor
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Inflammation/Immunology
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μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
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- HY-P1481
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-
- HY-P1467
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- HY-P3376
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- HY-P1502
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Opioid Receptor
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Neurological Disease
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β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
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- HY-P1013
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- HY-P1333
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
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- HY-P10006
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Opioid Receptor
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Neurological Disease
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Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .
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- HY-P1333A
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Opioid Receptor
Apoptosis
Caspase
Endogenous Metabolite
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Neurological Disease
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Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
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- HY-P1470
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- HY-P1336
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- HY-P1337
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- HY-P1013A
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- HY-P3445
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- HY-P3445A
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- HY-P1481A
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- HY-P1337A
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- HY-P0088
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Dynorphin A Porcine Fragment 1-13
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Opioid Receptor
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Others
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Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
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- HY-P1577
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- HY-P0244
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- HY-P2018
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- HY-P3517
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β-EP (6-31), human
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Opioid Receptor
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Neurological Disease
Endocrinology
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β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
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- HY-P0210
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DAMGO
4 Publications Verification
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Opioid Receptor
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Cancer
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DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-P0244A
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- HY-P3555
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- HY-P3870
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Opioid Receptor
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Neurological Disease
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DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects .
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- HY-P3870A
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Opioid Receptor
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Neurological Disease
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DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
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- HY-P10394
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- HY-P3609
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JNJ 38488502; FE 200665
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Opioid Receptor
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Neurological Disease
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CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
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- HY-P0210B
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Opioid Receptor
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Cancer
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DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR .
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- HY-P3555A
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Opioid Receptor
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Others
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D-Ala-Gly-Phe-Met-NH2 monoacetate, an opioid peptide, is a potent opiate δ-receptor agonist .
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- HY-P1198
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia .
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- HY-P3870B
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Opioid Receptor
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Neurological Disease
|
DALDA TFA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA TFA shows antinociceptive and respiratory effects .
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- HY-P3043
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Opioid Receptor
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Neurological Disease
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Bilaid A is a μ-opioid receptor agonist that can be extracted from Penicillium. The Ki value is 3.1 μM. Bilaid A can be used in pain research .
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- HY-P1170
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Ac-L-Tyr-Gly-Gly-L-Phe-D-Leu-COOH
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Opioid Receptor
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Neurological Disease
|
N-terminally acetylated Leu-enkephalin is the N-terminally acetylated form of Leu-enkephalin. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
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- HY-P1198A
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Neurokinin Receptor
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Neurological Disease
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Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia .
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- HY-P0288
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Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin
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Opioid Receptor
Endogenous Metabolite
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Neurological Disease
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[Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
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- HY-P1317
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Opioid Receptor
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Neurological Disease
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Nociceptin (1-13), amide is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes .
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- HY-P1317A
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Opioid Receptor
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Neurological Disease
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Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes .
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- HY-P0186
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Opioid Receptor
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Neurological Disease
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Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
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- HY-P1332
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[D-Ser2, Leu5, Thr6]-enkephalin
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Opioid Receptor
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Neurological Disease
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DSLET ([D-Ser2, Leu5, Thr6]-enkephalin) is a highly specific agonist of the δ-receptor. DSLET is an enkephalin-related peptide selectively bound to the δ opioid receptor .
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- HY-P0288A
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- HY-P0186A
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Opioid Receptor
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Neurological Disease
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Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
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- HY-129271
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Deltorphin A; Dermenkephalin
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Opioid Receptor
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Others
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Deltorphin (Deltorphin A; Dermenkephalin) is a biological active peptide. (Deltorphin A peptide was isolated from skin extracts of the South American frog, Phyllomedusa sauvagei. Deltorphin A is a potent and selective agonist for the delta-opioid receptor.)
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- HY-P3647
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- HY-P3647A
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Opioid Receptor
Adenylate Cyclase
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Neurological Disease
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[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .
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- HY-P1316
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Opioid Receptor
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Neurological Disease
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Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
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- HY-P1316A
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Opioid Receptor
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Neurological Disease
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Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
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- HY-17609
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CR-845; FE-202845
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Opioid Receptor
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Neurological Disease
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Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
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- HY-P1338
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Opioid Receptor
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Neurological Disease
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PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
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- HY-P4107
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Opioid Receptor
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Neurological Disease
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Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr) .
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- HY-P0185
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Opioid Receptor
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Neurological Disease
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Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
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- HY-P1338A
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Opioid Receptor
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Neurological Disease
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PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
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- HY-P0185A
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Opioid Receptor
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Neurological Disease
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Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
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- HY-P4053
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Opioid Receptor
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Neurological Disease
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Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity .
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- HY-P3044
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Opioid Receptor
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Neurological Disease
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Bilaid A1e (Compound 1e) is a tetrapeptide agonist of the µ-opioid receptor (Ki = 750 nM). Bilaid A1e can be isolated from an Australian estuarine isolate of Penicillium sp. Bilaid A1e can be used for pain research .
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- HY-P3634
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Opioid Receptor
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Neurological Disease
|
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .
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- HY-P1301
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Opioid Receptor
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Neurological Disease
|
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
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- HY-P1301A
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Opioid Receptor
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Neurological Disease
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[Arg14,Lys15]Nociceptin TFA is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin TFA displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
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- HY-P1626
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Opioid Receptor
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Neurological Disease
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Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway .
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- HY-P4679
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E2078
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Opioid Receptor
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Neurological Disease
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(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .
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- HY-P1300
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Opioid Receptor
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Neurological Disease
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[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold) .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0418AS
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Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
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- HY-G0021S1
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N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
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-
- HY-123689S
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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-
- HY-123689S1
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Samidorphan-d5 (ALKS-33-d5) is a tritiated version of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
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- HY-G0021S
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N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
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- HY-B1052S
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Lofexidine-d4 (hydrochloride) (Baq-168-d4) is the deuterium labeled Lofexidine hydrochloride. Lofexidine hydrochloride is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
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