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-118949
    LY255582
    		Antagonist 98.0%
    LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity.
    LY255582
  • HY-141515
    BMS-986121
    		Modulator 99.96%
    BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs.
    BMS-986121
  • HY-P1334A
    DPDPE TFA
    		Agonist 99.81%
    DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.
    DPDPE TFA
  • HY-P1596
    Gluten Exorphin C
    		Inhibitor 99.86%
    Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
    Gluten Exorphin C
  • HY-126941
    Hecogenin acetate
    		98.57%
    Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
    Hecogenin acetate
  • HY-101223
    DIPPA hydrochloride
    		Antagonist 99.7%
    DIPPA hydrochloride is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA hydrochloride can be used for the research of anxiety and antidepressant.
    DIPPA hydrochloride
  • HY-P4053
    Dalargin
    		Agonist 99.52%
    Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin (HY-A0276A)-induced kidney injury. Dalargin shows antiulcer activity.
    Dalargin
  • HY-156131
    Loperamide
    		Agonist 99.85%
    Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent.
    Loperamide
  • HY-107749
    ML 190
    		Antagonist 99.60%
    ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively.
    ML 190
  • HY-108229S
    6β-Naltrexol-d3
    		Antagonist 99.72%
    6β-Naltrexol-d3 (6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit.
    6β-Naltrexol-d<sub>3</sub>
  • HY-P1013
    Deltorphin 2
    		Agonist
    Deltorphin 2 is a selective peptide agonist for the δ opioid receptor.
    Deltorphin 2
  • HY-123534
    CYT-1010
    		Agonist 99.74%
    CYT-1010 is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
    CYT-1010
  • HY-100845
    Salvinorin A
    		Inhibitor 98.99%
    Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with Ki value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.
    Salvinorin A
  • HY-15997C
    (±)-U-50488 hydrate hydrochloride
    		Agonist 99.76%
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (±)-U-50488 hydrate hydrochloride
  • HY-110302
    6'-GNTI dihydrochloride
    		Agonist 99.54%
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
    6'-GNTI dihydrochloride
  • HY-112692
    AT-121
    		Agonist 99.73%
    AT-121 is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.
    AT-121
  • HY-101317
    TAN-67 dihydrobromide
    		Agonist 99.20%
    TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke.
    TAN-67 dihydrobromide
  • HY-P1793A
    α-Casein (90-95) TFA
    		Agonist 99.58%
    α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) TFA inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) TFA activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer.
    α-Casein (90-95) TFA
  • HY-118416
    BMS-986124
    		Antagonist 99.00%
    BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM).
    BMS-986124
  • HY-B0418AS
    Loperamide-d6 hydrochloride
    		Agonist 99.10%
    Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea.
    Loperamide-d<sub>6</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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