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-107722
    SCH 221510
    		Agonist 99.00%
    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.
    SCH 221510
  • HY-107748
    5'-Guanidinonaltrindole hydrochloride
    		Antagonist 98.72%
    5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor.
    5'-Guanidinonaltrindole hydrochloride
  • HY-15708
    LY2795050
    		Antagonist 98.12%
    LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.
    LY2795050
  • HY-P1470
    [Leu5]-Enkephalin, amide
    		Agonist 99.76%
    [Leu5]-Enkephalin, amide is a δ opioid receptor agonist.
    [Leu5]-Enkephalin, amide
  • HY-101230
    ICI 174864
    		99.97%
    ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom.
    ICI 174864
  • HY-P0185A
    Endomorphin 1 acetate
    		Agonist 99.92%
    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.
    Endomorphin 1 acetate
  • HY-101079
    BRL 52537 hydrochloride
    		Agonist 98.14%
    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.
    BRL 52537 hydrochloride
  • HY-124959
    Spiradoline mesylate
    		Agonist 99.95%
    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.
    Spiradoline mesylate
  • HY-P1170
    N-terminally acetylated Leu-enkephalin
    		Agonist 99.49%
    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.
    N-terminally acetylated Leu-enkephalin
  • HY-114452A
    LY2940094 tartrate
    		Antagonist 99.66%
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
    LY2940094 tartrate
  • HY-145404
    Mitragynine pseudoindoxyl
    		Agonist 99.9%
    Mitragynine pseudoindoxyl is a potent MOR agonist. Mitragynine pseudoindoxyl displays reduced hyperlocomotion, inhibition of GI transit and reinforcing properties.
    Mitragynine pseudoindoxyl
  • HY-113316A
    (±)-Salsolinol hydrochloride
    		Agonist 98%
    (±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioid receptors (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).
    (±)-Salsolinol hydrochloride
  • HY-P3445A
    Anrikefon acetate
    		Agonist 99.25%
    Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect.
    Anrikefon acetate
  • HY-P1866A
    β-Endorphin, equine TFA
    		Agonist
    β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. β-Endorphin, equine TFA has analgesic properties.
    β-Endorphin, equine TFA
  • HY-101039A
    AR-M 1000390 hydrochloride
    		Agonist 98.20%
    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.
    AR-M 1000390 hydrochloride
  • HY-P1317A
    Nociceptin (1-13), amide TFA
    		Agonist 99.87%
    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.
    Nociceptin (1-13), amide TFA
  • HY-16765A
    Axelopran sulfate
    		Antagonist 99.14%
    Axelopran sulfate is an opioid receptor 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.
    Axelopran sulfate
  • HY-P1335
    CTAP
    		Antagonist 99.30%
    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-107094
    MT-7716 hydrochloride
    		Agonist 99.06%
    MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
    MT-7716 hydrochloride
  • HY-120949
    (1R,2R)-U-50488 hydrochloride
    		Agonist 99.14%
    (1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (1R,2R)-U-50488 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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