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 (142):

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-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-15122A
    Sinomenine hydrochloride Activator 99.88%
    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-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-P1299A
    UFP-101 TFA Antagonist 99.36%
    UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
  • HY-120645
    BMS-986122 Agonist ≥98.0%
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes.
  • HY-A0118
    Naloxegol Antagonist
    Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
  • 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-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-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-P0288
    [Leu5]-Enkephalin Agonist 99.81%
    [Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
  • HY-P0183
    Nociceptin Agonist 99.83%
    Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
  • 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-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-100903
    Norbinaltorphimine dihydrochloride Antagonist 99.04%
    Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
  • HY-124754
    BTRX-335140 Inhibitor 99.71%
    BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) .
  • HY-101386
    PZM21 Agonist 99.84%
    PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
  • HY-P0073
    Tyr-Gly-Gly-Phe-Met-OH Activator 98.07%
    Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
  • 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.
Isoform Specific Products

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