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μopioidreceptor agonist 3 (compound 20) is a potent μopioidreceptor (µOR) agonist with an EC50 of 0.87 nM. μopioidreceptor agonist 3 has the potential for pain and neuropsychiatric indications research .
μopioidreceptor agonist 2 （Compound H-3）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MORreceptor agonist and can be used for the research of pain and pain related diseases .
μopioidreceptor agonist 1 （Compound H-1a）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MORreceptor agonist and can be used for the research of pain and pain related diseases .
Muopioidreceptor antagonist 4 (compound 31) is a potent and selective μopioidreceptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Muopioidreceptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Muopioidreceptor antagonist 4 Muopioidreceptor antagonist 4 can be used for researching opioid use disorders (OUD) .
Muopioidreceptor antagonist 3 (compound 26) is a potent and selective μopioidreceptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Muopioidreceptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Muopioidreceptor antagonist 3 can be used for researching opioid use disorders (OUD) .
Muopioidreceptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μopioidreceptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Muopioidreceptor antagonist 5 can be used for researching opioid use disorders (OUD) .
Muopioidreceptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μopioidreceptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Muopioidreceptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Muopioidreceptor antagonist 2 can be used for researching opioid use disorders (OUD) .
σ1 Receptor/μOpioidreceptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μopioidreceptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μOpioidreceptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μOpioidreceptor modulator 1 can be used for the research of neuropathic pain .
Muopioidreceptor antagonist 8 (368) is a μ-opioidreceptor antagonist. Muopioidreceptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
Muopioidreceptor antagonist 1 (compound 19) is a selective and orally active μopioidreceptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Muopioidreceptor antagonist 1 increases intestinal motility during morphine-induced constipation. Muopioidreceptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
Muopioidreceptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioidreceptor), with an IC50 of 29 ± 3.0 nM. Muopioidreceptor antagonist 7 can be used for the research of pain and opioid use disorder .
μ/κ/δ opioidreceptor agonist 1 is a μopioidreceptor (MOR), κ opioidreceptor (KOR), and δ opioidreceptor (DOR) agonist. μ/κ/δ opioidreceptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μopioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
PL-017 is a potent and selective μopioidreceptor 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 .
PL-017 TFA is a potent and selective μopioidreceptor 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 .
Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioidreceptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan hydrochloride primarily acts as an opioidreceptor antagonist in vivo .
Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
Alvimopan metabolite is a μopioidreceptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μopioidreceptor antagonist during research and development .
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioidreceptors. Samidorphan acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan primarily acts as an opioidreceptor antagonist in vivo .
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
NAQ is a potent and selective μopioidreceptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Muopioidreceptor 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 .
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‐opioidreceptors. Samidorphan acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan primarily acts as an opioidreceptor antagonist in vivo .
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioidreceptors. Samidorphan is a μ-opioidreceptor antagonist and a partial agonist at k-opioid and δ-opioidreceptors. Samidorphan acts primarily as an opioidreceptor antagonist in vivo .
Loperamide (ADL 2-1294) is a selective μopioidreceptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioidreceptor, respectively. Loperamide can be used as an antidiarrheal agent .
3-Carboxamidonaltrexone (example 32) is a opioidreceptor binding compound with Ki values of 1.9 nM, 110 nM, and 22 nM for μ-opioidreceptor, δ-opioidreceptor, and K-opioidreceptor, respectively .
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μopioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Cyprodime hydrochloride is a highly selective μ-opioidreceptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioidreceptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect .
Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation[1][2].
Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors .
SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioidreceptor partial agonist, with high binding affinity (NOP receptorKi=7.49; μ-OpioidreceptorKi=2.70). SR-16435 can relieve pain .
Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus .
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioidreceptor agonist, and a partial agonist at the cloned μ and δ opioidreceptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect .
BMS-986121 is a positive allosteric modulator (PAM) of the μopioidreceptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μreceptor PAMs .
AP-238 is a a new synthetic opioid (NSO), and acts as an agonist for μ-opioidreceptor (MOR) with an EC50 of 248 nM. AP-238 exhibits analgesic activity .
Isotodesnitazene is a kind of opioids. Isotodesnitazene primarily acts on μ-opioidreceptors (MOR). Isotodesnitazene has an EC50 of 34.8 nM for MOR-βarr2 and 142 nM for MOR-mini-Gi. Isotodesnitazene can be used in the study of opioids .
CYM51010 is a biased ligand of μ-opioidreceptor – δ-opioidreceptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
Axelopran sulfate is an opioidreceptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
DALDA acetate is a potent and highly selective μ-opioidreceptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioidreceptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Bromadoline maleate is an opioid analgesic selective for the μ-opioidreceptor, exhibiting analgesic activity in various biological fluids. Bromadoline maleate has been successfully quantified alongside its N-demethylated metabolites in human and canine samples.
Axelopran (TD-1211) is an opioidreceptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioidreceptor (KOR) agonist, and is also an agonist for other opioidreceptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
BNTX (7-Benzylidenenaltrexone) maleate is a δ1-opioidreceptor antagonist with the Kis of 0.1, 10.8, 13.3, and 58.6 nM for δ1, δ2-, μ-, and κ-opioidreceptor, respectively. BNTX maleate shows antinociceptive activity .
Biocytin-β-endorphin, human is abiotinylated β-Endorphin, human (HY-P1502). β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
LY2048978 is a non-selective opioidreceptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioidreceptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder .
AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioidreceptors, with Ki values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively .
Naloxonazine dihydrochloride is a specific μ-opioidreceptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity .
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 opioidreceptor (KOR) agonist, and is also an agonist for other opioidreceptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioidreceptors. β-Endorphin, equine TFA has analgesic properties .
MOR modulator-1 (compound 6) is a potent and selective μopioidreceptor (MOR) modulator. MOR modulator-1 exhibits improved opioidreceptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Ki of 0.25, 41.1, 1.30 nM, respectively[1]
Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioidreceptors over the δ-opioidreceptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioidreceptors (IC50s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.
DPI-3290 (Org 41793) is a potent and specific opioidreceptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioidreceptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .
GSK1521498 is a potent and selective μ-opioidreceptor (MOR) antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents .
Naldemedine (S-297995) tosylate is an orally active μ-opioidreceptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioidreceptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
Naldemedine (S-297995) is an orally active μ-opioidreceptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioidreceptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
β-Endorphin, an endogenous opioid neuropeptide, is an opioidreceptor agonist. β-Endorphin binds preferentially to μ-opioidreceptors 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 .
Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioidreceptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
Atoxifent is a potent μ-opioidreceptor 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 .
Naltriben mesylate is a potent δ2-opioidreceptor antagonist and a TRPM7 activator. Naltriben mesylate shows Ki values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer .
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
CTAP is a potent, highly selective, and BBB penetrant μopioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
R(+)-6-Bromo-APB hydrobromide is a dopamine (DA) agonist. R(+)-6-Bromo-APB hydrobromide increased the expression of µ opioidreceptor (MOR) mRNA in the nucleus accumbens .
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
GSK1521498 free base is a potent and selective μ-opioidreceptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents .
Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioidreceptor (KOR) agonist, and is also an agonist for other opioidreceptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
GSK1521498 free base (hydrochloride) is a potent and selective μ-opioidreceptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents .
CTAP TFA is a potent, highly selective, and BBB penetrant μopioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
AT-121 is a bifunctional nociception and muopioidreceptor 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 .
AT-121 hydrochloride is a bifunctional nociception and muopioidreceptor 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 .
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-opioidreceptor via an endorphin-like pathway .
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioidMu-1 receptor (Ki = 2.7 μM) .
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioidreceptors. UFP-101 shows antidepressant-like effect .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
CYT-1010 hydrochloride is a mu-opioidreceptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .
CYT-1010 is a mu-opioidreceptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .
Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
MOR agonist-1 is a MOR (μ-opioidreceptor) agonist. MOR agonist-1 has good analgesic effect. MOR agonist-1 can be used for the research of pain and pain-related disorders .
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioidreceptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioidreceptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioidreceptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .
CP-866,087 is a novel, potent and selective μ-opioidreceptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .
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-OpioidReceptor (MOPr) agonist (Ki=210 nM, hMOPr) .
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-opioidreceptors .
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioidreceptor(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 .
(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioidreceptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum .
Fluorphine is an analogue of Brorphine and can bind to μ-opioidreceptor (MOR) (Ki: 12.5 nM). Fluorphine has GTPγS binding (EC50: 75 nM) and βarrestin 2 recruitment (EC50: 377 nM) activity. Fluorphine induces respiratory depressant effects .
CTOP is a potent and highly selective μ-opioidreceptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioidreceptors(µ-opioidreceptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
BMS-986187 is an δ-opioidreceptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB?of 6.02 (～1?μM). BMS-986187 has no observable PAM activity at the?μ-receptor (EC50=3 μM) .
TAN-452 is an orally active, selective peripherally acting δ-opioidreceptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioidreceptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioidreceptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioidreceptor (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 .
Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioidreceptor, with analgesic effect .
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioidreceptor (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 .
BPR1M97 is a dual-acting muopioidreceptor (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 .
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioidreceptor (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 .
HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioidreceptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model .
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioidreceptors. UFP-101 TFA shows antidepressant-like effect .
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioidreceptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
BRL 52537 hydrochloride is a highly selective κ-Opioidreceptor (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 .
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioidreceptor (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 .
α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioidreceptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling .
LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappareceptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity .
BU09059 is a potent and selective Kappa-opioidreceptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
KOR agonist 4 (compound 39) is an agonist of Kappa OpioidReceptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioidreceptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
RO-76 is a muopioidreceptor (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 .
[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 opioidreceptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
[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 opioidreceptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
(±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioidreceptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA) .
O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioidreceptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
MOR agonist-3 (Compound 84) is a D3R/MOR antagonist/partial agonist a(Ki 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioidreceptor) (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 .
KNT-127 is a potent δ-opioidreceptor agonist that crosses the blood-brain barrier (BBB). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 has analgesic, antidepressant and antianxiety activities .
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioidreceptor (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 .
[(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 μopioidreceptors (>3000 fold) .
[(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 μopioidreceptors (>3000 fold) .
(RS)-Salsolinol hydrobromide is the hydrobromide form of (±)-Salsolinol (HY-113316). (RS)-Salsolinol hydrobromide is a Dopamine (HY-B0451)-derived endogenous metabolite. (RS)-Salsolinol hydrobromide activates μ-opioidreceptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA) .
BPRMU191 is a μ-opioidreceptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioidreceptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioidreceptor (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) .
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-opioidreceptor (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 .
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioidreceptor 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 .
(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioidreceptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs .
RS 39604 is a potent, selective, and orally active 5-HT4receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioidmureceptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
CP-96021 is a potent and orally available leukotriene D4 (LTD4Ki=34 μM) / platelet activating factor (PAFKi=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μopioid, and GABAreceptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma .
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
μ/κ/δ opioidreceptor agonist 1 is a μopioidreceptor (MOR), κ opioidreceptor (KOR), and δ opioidreceptor (DOR) agonist. μ/κ/δ opioidreceptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μopioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
PL-017 is a potent and selective μopioidreceptor 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 .
PL-017 TFA is a potent and selective μopioidreceptor 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 .
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μopioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
DALDA acetate is a potent and highly selective μ-opioidreceptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioidreceptor (KOR) agonist, and is also an agonist for other opioidreceptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
Biocytin-β-endorphin, human is abiotinylated β-Endorphin, human (HY-P1502). β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
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 opioidreceptor (KOR) agonist, and is also an agonist for other opioidreceptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioidreceptors. β-Endorphin, equine TFA has analgesic properties .
β-Endorphin, an endogenous opioid neuropeptide, is an opioidreceptor agonist. β-Endorphin binds preferentially to μ-opioidreceptors 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 .
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
CTAP is a potent, highly selective, and BBB penetrant μopioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioidreceptor (KOR) agonist, and is also an agonist for other opioidreceptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
CTAP TFA is a potent, highly selective, and BBB penetrant μopioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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-opioidreceptor via an endorphin-like pathway .
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioidreceptors. UFP-101 shows antidepressant-like effect .
β-Endorphin (1-27) (human) is an opioid antagonist that binds μ-, δ-, and κ-opioidreceptors with Kis of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .
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-OpioidReceptor (MOPr) agonist (Ki=210 nM, hMOPr) .
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-opioidreceptors .
CTOP is a potent and highly selective μ-opioidreceptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioidreceptor (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 .
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioidreceptors. UFP-101 TFA shows antidepressant-like effect .
α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioidreceptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling .
[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 opioidreceptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
[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 opioidreceptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively .
[(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 μopioidreceptors (>3000 fold) .
(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioidreceptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs .
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioidreceptors. β-Endorphin, equine TFA has analgesic properties .
(S)-Laudanosine is an alkaloid that can be found in poppies and is the S-enantiomer of Laudanosine. Laudanosine acts on the central nervous system and cardiovascular system, inhibiting low-affinity GABA receptors with an IC50 value of 10 μM, and can cause seizures, hypotension, and bradycardia. Additionally, Laudanosine exerts analgesic effects by competitively binding to the opioidMu-1 receptor (Ki = 2.7 μM) .
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioidreceptor, with analgesic effect .
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioidreceptor (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 .
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-opioidreceptor (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 .
The OPRM1 protein serves as a receptor for endogenous and synthetic opioids and undergoes conformational changes upon agonist binding, activating downstream signaling pathways. This includes coupling to G proteins, thereby regulating adenylyl cyclase, calcium channels, potassium channels, and intracellular signaling pathways. OPRM1 Protein, Human (Cell-Free, His) is the recombinant human-derived OPRM1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of OPRM1 Protein, Human (Cell-Free, His) is 400 a.a., with molecular weight of 47.6 kDa.
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‐opioidreceptors. Samidorphan acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan primarily acts as an opioidreceptor antagonist in vivo .
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioidreceptors. Samidorphan is a μ-opioidreceptor antagonist and a partial agonist at k-opioid and δ-opioidreceptors. Samidorphan acts primarily as an opioidreceptor antagonist in vivo .
Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation[1][2].
O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioidreceptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
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