2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Opioid Receptor

Opioid Receptor

Opioid Receptor

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Opioid receptors are a group of G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. Opioid receptors are distributed widely in the brain, and are found in the spinal cord and digestive tract. Opioid receptors are molecules, or sites, within the body that are activated by opioid substances. Opioid receptors inhibit the transmission of impulse in excitatory pathways within the human body system. These pathways include the serotonin, catecholamine, and substance P pathways, which are all implicated in pain perception and feelings of well-being. Opioid receptors are further subclassified into mu, delta, and kappa receptors. All the classes, while exhibiting differing modes of action, share some basic similarities. They all are driven by the potassium pump mechanism, which is found on the plasma membrane of the majority of cells.

Opioid Receptor Isoform Specific Products:

Opioid Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0210
    DAMGO
    		Agonist 99.90%
    DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR.
    DAMGO
  • HY-B0418A
    Loperamide hydrochloride
    		Agonist 99.90%
    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.
    Loperamide hydrochloride
  • HY-N0164
    Matrine
    		Agonist ≥98.0%
    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).
    Matrine
  • HY-101718
    Aticaprant
    		Antagonist 99.87%
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
    Aticaprant
  • HY-P0288
    [Leu5]-Enkephalin
    		Agonist 99.87%
    [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.
    [Leu5]-Enkephalin
  • HY-101302
    Naltriben mesylate
    		Antagonist 99.65%
    Naltriben mesylate is a potent δ2-opioid receptor 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.
    Naltriben mesylate
  • HY-15997
    (-)-U-50488 hydrochloride
    		Inhibitor 99.71%
    (-)-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).
    (-)-U-50488 hydrochloride
  • HY-15997B
    (±)-U-50488 hydrochloride
    		Agonist 99.73%
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (±)-U-50488 hydrochloride
  • HY-15122
    Sinomenine
    		Activator 99.94%
    Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
    Sinomenine
  • HY-15122A
    Sinomenine hydrochloride
    		Activator 98.67%
    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-opioid receptor.
    Sinomenine hydrochloride
  • HY-17417
    Naloxone hydrochloride
    		Antagonist 99.96%
    Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.
    Naloxone hydrochloride
  • HY-100903
    Norbinaltorphimine dihydrochloride
    		Antagonist 98.17%
    Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
    Norbinaltorphimine dihydrochloride
  • HY-P1333
    Dynorphin A
    		Agonist 98.06%
    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.
    Dynorphin A
  • HY-P0183
    Nociceptin
    		Agonist 98.70%
    Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
    Nociceptin
  • HY-P0073
    Tyr-Gly-Gly-Phe-Met-OH
    		Activator 99.80%
    Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
    Tyr-Gly-Gly-Phe-Met-OH
  • HY-10487
    JDTic dihydrochloride
    		Antagonist 98.01%
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
    JDTic dihydrochloride
  • HY-101202
    SNC80
    		Agonist 99.44%
    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.
    SNC80
  • HY-P1502
    β-Endorphin, human
    		Agonist
    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.
    β-Endorphin, human
  • HY-13274
    JTC-801
    		Antagonist 98.91%
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
    JTC-801
  • HY-B0557
    Bisacodyl
    		Inhibitor 99.59%
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
    Bisacodyl
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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