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-123534A
    CYT-1010 hydrochloride
    		Agonist
    CYT-1010 hydrochloride is a mu-opioid receptor 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 hydrochloride
  • HY-19876
    PL37
    		Agonist
    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-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain.
    PL37
  • HY-100845
    Salvinorin A
    		Inhibitor ≥98.0%
    Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.
    Salvinorin A
  • HY-113929R
    Loperamide oxide (Standard)
    		Agonist
    Loperamide oxide (Standard) is the analytical standard of Loperamide oxide. This product is intended for research and analytical applications. Loperamide oxide (R-58425) is a orally active prodrug of the Loperamide (HY-156131). Loperamide oxide incubation with the contents of the intestinal lumen inhibits fluid secretion under aerobic conditions.
    Loperamide oxide (Standard)
  • HY-107747A
    GR 89696 free base
    		Agonist
    GR 89696 free base is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.
    GR 89696 free base
  • HY-115066A
    GSK1521498 free base (hydrochloride)
    		Antagonist
    GSK1521498 free base (hydrochloride) is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498 free base (hydrochloride)
  • HY-P1335
    CTAP
    		Antagonist
    CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor 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.
    CTAP
  • HY-128038
    N-Desmethyl-loperamide
    		Activator
    N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein.
    N-Desmethyl-loperamide
  • HY-P1338A
    PL-017 TFA
    		Agonist
    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.
    PL-017 TFA
  • HY-156614
    Icalcaprant
    		Antagonist
    Icalcaprant is a kappa-opioid receptor antagonist.
    Icalcaprant
  • HY-106732
    AT-076
    		Antagonist
    AT-076 is an opioid pan antagonist at nociception, kappa, mu, and delta opioid receptors, with Ki values of 1.75 nM (NOP), 1.67 nM (MOP), 1.14 nM (KOP) and 19.6 nM (DOP), respectively.
    AT-076
  • HY-P0288A
    [Leu5]-Enkephalin TFA
    		Agonist
    [Leu5]-Enkephalin TFA is a pentapeptide with morphine like properties. [Leu5]-Enkephalin TFA is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
    [Leu5]-Enkephalin TFA
  • HY-145128
    GR103545
    		Agonist
    GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). 11GR103545 is a radiotracer for imaging κ-OR in vivo[1]
    GR103545
  • HY-169450
    (-)-9-Hydroxycorynantheidine
    		Agonist
    (-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioid receptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum.
    (-)-9-Hydroxycorynantheidine
  • HY-139678
    SC13
    		Agonist
    SC13 is a novel mitragynine analog with low-efficacy Mu opioid receptor agonism that displays antinociception with attenuated adverse effects.
    SC13
  • HY-P1779A
    β-Casomorphin (1-5), bovine TFA
    β-Casomorphin (1-5), bovine (TFA) is a peptide of bovine β-Casomorphin.
    β-Casomorphin (1-5), bovine TFA
  • HY-136586
    Loperamide phenyl
    		Antagonist
    Loperamide phenyl is an impurity of Loperamide (HY-B0418A). Loperamide is an opioid receptor agonist.
    Loperamide phenyl
  • HY-P1171
    N-terminally acetylated Endomorphin-1
    		Control 99.20%
    N-terminally acetylated Endomorphin-1 is a modified Endomorphin-1.
    N-terminally acetylated Endomorphin-1
  • HY-163916
    SalA-VS-07
    		Agonist
    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.
    SalA-VS-07
  • HY-P1502F
    Biocytin-β-endorphin, human
    		Agonist
    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 opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
    Biocytin-β-endorphin, human
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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