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 (122):

Cat. No. Product Name Effect Purity
  • HY-P0210
    DAMGO Agonist 99.13%
    DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR.
  • HY-101177
    Naltrindole hydrochloride Antagonist
    Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM.
  • HY-B0418A
    Loperamide hydrochloride Agonist 99.79%
    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.
  • 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-12745A
    Nalfurafine hydrochloride Agonist 99.93%
    Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-P1335A
    CTAP TFA Antagonist
    CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and 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).
  • HY-100903
    Norbinaltorphimine dihydrochloride Antagonist 98.60%
    Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
  • HY-13101
    MCOPPB triHydrochloride Agonist 99.35%
    MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
  • HY-15122A
    Sinomenine hydrochloride Activator 99.46%
    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.
  • HY-101718
    Aticaprant Antagonist 99.86%
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
  • 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-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-101386
    PZM21 Agonist 99.57%
    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  • HY-P0288
    [Leu5]-Enkephalin Agonist 99.81%
    [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 99.75%
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
  • 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-15536
    Cebranopadol Agonist
    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-P0183
    Nociceptin Agonist 99.83%
    Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
  • HY-P0185
    Endomorphin 1 Agonist
    Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
  • 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.
Isoform Specific Products

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