1. GPCR/G Protein
    Neuronal Signaling
  2. 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 (55):

Cat. No. Product Name Effect Purity
  • HY-101386
    PZM21 Agonist 99.45%
    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  • HY-B0418A
    Loperamide hydrochloride Agonist 99.69%
    Loperamide hydrochloride is an opiate receptor agonist for the treatment of diarrhea.
  • HY-13044
    ADL-5859 Agonist 99.65%
    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 98.66%
    N-Desmethylclozapine is a dengue virus inhibitor, and an agonist of δ-opioid receptor.
  • 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-10827
    Kelatorphan Inhibitor
    Kelatorphan is a full inhibitor of enkephalin degrading enzymes.
  • HY-75766AS
    Methylnaltrexone D3 iodide
    Methylnaltrexone D3 iodide is the deuterium labeled Methylnaltrexone iodide. Methylnaltrexone iodide is a peripheral-acting opioid receptor antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.
  • HY-P1594A
    Dynorphin A (1-10) TFA Agonist
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM. Sequence: Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro;YGGFLRRIRP.
  • HY-10487
    JDTic dihydrochloride Antagonist 98.18%
    JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
  • HY-101718
    CERC-501 Antagonist 99.24%
    LY-2456302 is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
  • HY-13274
    JTC-801 Antagonist 99.20%
    JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 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 Sequence: Tyr-Gly-Gly-Phe-Met;YGGFM.
  • HY-N0164
    Matrine >98.0%
    Matrine(Sophocarpidine; α-Matrine) is an alkaloid found in plants from the Sophora genus.
  • HY-15536
    Cebranopadol Agonist 98.24%
    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. Sequence: Tyr-Gly-Gly-Phe-Leu;YGGFL.
  • 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-P0210
    DAMGO Agonist 98.10%
    DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist. Sequence: Tyr-{d-Ala}-Gly-{Me-Phe}-Gly-ol;Y-{d-Ala}-G-{Me-Phe}-G-ol.
  • HY-P0183
    Nociceptin Agonist 99.79%
    Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Sequence: Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Leu-Ala-Asn-Gln;FGGFTGARKSARKLANQ.
  • HY-111454
    SR17018 Agonist >98.0%
    SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
  • HY-P0185
    Endomorphin 1 Agonist 98.15%
    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. Sequence: Tyr-Pro-Trp-Phe-NH2;YPWF-NH2.