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-114452A
    LY2940094 tartrate
    		Antagonist 99.66%
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
    LY2940094 tartrate
  • HY-15708
    LY2795050
    		Antagonist 98.12%
    LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.
    LY2795050
  • HY-145404
    Mitragynine pseudoindoxyl
    		Modulator 99.9%
    Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic.
    Mitragynine pseudoindoxyl
  • HY-109054A
    O-Desmethyltramadol hydrochloride
    		Agonist 99.79%
    O-Desmethyltramadol hydrochloride is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol hydrochloride mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR).
    O-Desmethyltramadol hydrochloride
  • HY-176710
    PAD-PF2
    		Agonist 99.94%
    PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC50 = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC50 = 12.3 μM). The IC50 values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca2+-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer.
    PAD-PF2
  • HY-N2571
    Corydine
    		Agonist 99.93%
    Corydine is a HIV-1 reverse transcriptase inhibitor and μ-opioid receptor (MOR) agonist, with an IC50 of 356.7 μg/mL against HIV-1 reverse transcriptase, an EC50 of 0.51 μM for MOR, and a Ki of 2.82 μM for MOR. Corydine produces antinociceptive effects by inhibiting acetic acid-induced writhing behavior in a MOR-dependent manner. Corydine inhibits the proliferation of cancer cells, mitogen-stimulated lymphocytes and IL-2-dependent cells. Corydine can be used in studies related to human immunodeficiency virus infection, visceral pain, leukemia, melanoma, bladder cancer and colon adenocarcinoma.
    Corydine
  • HY-128865
    BPR1M97
    		Agonist 99.42%
    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.
    BPR1M97
  • 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-168366
    R-6890
    		Antagonist 99.59%
    R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC50=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats.
    R-6890
  • HY-136832
    Noribogaine hydrochloride
    		Modulator 99.9%
    Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity.
    Noribogaine hydrochloride
  • HY-P1317A
    Nociceptin (1-13), amide TFA
    		Agonist 99.87%
    Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.
    Nociceptin (1-13), amide TFA
  • HY-16765A
    Axelopran sulfate
    		Antagonist 99.14%
    Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.
    Axelopran sulfate
  • 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-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-101039A
    AR-M 1000390 hydrochloride
    		Agonist 98.20%
    AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
    AR-M 1000390 hydrochloride
  • HY-P4053
    Dalargin
    		Agonist 98.12%
    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-P0185A
    Endomorphin 1 acetate
    		Agonist 99.92%
    Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties.
    Endomorphin 1 acetate
  • HY-P1337A
    Dynorphin B (1-13) TFA
    		Agonist 99.58%
    Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor.
    Dynorphin B (1-13) TFA
  • HY-161405
    NPFF1-R antagonist 1
    		99.38%
    NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.
    NPFF1-R antagonist 1
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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