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

Opioid Receptor

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 Related Products (77):

Cat. No. Product Name Effect Purity
  • HY-12745A
    Nalfurafine hydrochloride Agonist 99.93%
    Nalfurafine hydrochloride is a κ-opioid agonist and an anti-itch drug approved in Japan.
  • HY-P0210
    DAMGO Agonist 98.10%
    DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR.
  • HY-B0418A
    Loperamide hydrochloride Agonist 99.69%
    Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist for the treatment of diarrhea. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.
  • HY-101386
    PZM21 Agonist 99.45%
    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  • HY-101177
    Naltrindole hydrochloride Antagonist 99.68%
    Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.
  • HY-P1467A
    [Met5]-Enkephalin, amide TFA Agonist 99.71%
    [Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.
  • HY-128865
    BPR1M97 Agonist
    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-N0164
    Matrine Agonist >98.0%
    Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.
  • HY-13044
    ADL-5859 Agonist 99.77%
    ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel.
  • HY-G0021
    N-Desmethylclozapine Agonist 99.72%
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug 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-10487
    JDTic dihydrochloride Antagonist 99.79%
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
  • HY-15122A
    Sinomenine hydrochloride Activator >98.0%
    Sinomenine hydrochloride is a blocker of the NF-κB activation and also an activator of μ-opioid receptor.
  • HY-101718
    Aticaprant Antagonist 99.24%
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
  • HY-15536
    Cebranopadol Agonist 98.76%
    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.
  • HY-P0288
    [Leu5]-Enkephalin Agonist 99.72%
    [Leu5]-Enkephalin is a pentapeptides with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
  • HY-13274
    JTC-801 Antagonist 99.73%
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
  • HY-P0183
    Nociceptin Agonist 99.79%
    Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
  • HY-P0073
    Tyr-Gly-Gly-Phe-Met-OH Activator 99.81%
    Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
  • HY-13222
    BAN ORL 24 Antagonist
    BAN ORL 24 is a potent and selective NOP receptor antagonist. (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively).
  • HY-111454
    SR17018 Agonist >98.0%
    SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
Isoform Specific Products

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