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-120456
    SR16835
    		Agonist
    SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect.
    SR16835
  • HY-P1301
    [Arg14,Lys15]Nociceptin
    		Agonist
    [Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
    [Arg14,Lys15]Nociceptin
  • HY-G0021S1
    N-Desmethylclozapine-d8 hydrochloride
    		Agonist 99.74%
    N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride 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 hydrochloride is also a δ-opioid agonist[1][2][3].
    N-Desmethylclozapine-d<sub>8</sub> hydrochloride
  • HY-P3647
    [DPro10] Dynorphin A (1-11), porcine
    		Agonist
    [DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property.
    [DPro10] Dynorphin A (1-11), porcine
  • HY-162669
    Mu opioid receptor antagonist 8
    		Antagonist
    Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi.
    Mu opioid receptor antagonist 8
  • HY-P3376
    Riminkefon
    		Agonist
    Riminkefon is a kappa opioid receptor agonist.
    Riminkefon
  • HY-136654
    LPK-26 hydrochloride
    		Agonist
    LPK-26 hydrochloride is a selective kappa-opioid receptor agonist with a Ki of 0.68 nM. LPK-26 exhibits potent antinociceptive effects with low physical dependence potential and can be utilized in relevant research.
    LPK-26 hydrochloride
  • HY-101306
    Clocinnamox mesylate
    Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors.
    Clocinnamox mesylate
  • HY-P3044
    Bilaid A1e
    		Agonist
    Bilaid A1e (Compound 1e) is a tetrapeptide agonist of the µ-opioid receptor (Ki = 750 nM). Bilaid A1e can be isolated from an Australian estuarine isolate of Penicillium sp. Bilaid A1e can be used for pain research.
    Bilaid A1e
  • HY-10672
    Urotensin-II receptor antagonist-1
    		Inhibitor
    Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM).
    Urotensin-II receptor antagonist-1
  • HY-14742
    Faxeladol
    Faxeladol is a compound with analgesic activity that reduced mean pain intensity compared with placebo in a suppression trial for painful polyneuropathy with a favorable safety profile.
    Faxeladol
  • HY-118615
    LY2048978
    		Antagonist
    LY2048978 is a non-selective opioid receptor antagonist with Ki of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder.
    LY2048978
  • HY-P3548
    [D-Ala2]-Met-Enkephalinamide
    		Agonist
    [D-Ala2]-Met-Enkephalinamide, an opioid peptide, is a potent opioid agonist. [D-Ala2]-Met-Enkephalinamide decreases bile flow by a central mechanism. [D-Ala2]-Met-Enkephalinamide has analgesic properties.
    [D-Ala2]-Met-Enkephalinamide
  • HY-144610
    Mu opioid receptor antagonist 5
    		Antagonist
    Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).
    Mu opioid receptor antagonist 5
  • HY-P3223
    Biphalin TFA
    Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent.
    Biphalin TFA
  • HY-158236
    ORL1 antagonist 2
    		Antagonist
    ORL1 antagonist 2 (1B) is an opioid receptor-Like 1 (ORL1) antagonist, usd in P-glycoprotein (P-gp) research.
    ORL1 antagonist 2
  • HY-142918
    μ opioid receptor agonist 1
    		Agonist
    μ opioid receptor agonist 1 （Compound H-1a）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases.
    μ opioid receptor agonist 1
  • HY-P1331
    BAM-22P
    		Agonist
    BAM-22P, a highly potent opioid peptide, is a potent opioid agonist.
    BAM-22P
  • HY-P3555
    D-Ala-Gly-Phe-Met-NH2
    		Agonist
    D-Ala-Gly-Phe-Met-NH2, an opioid peptide, is a potent opiate δ-receptor agonist.
    D-Ala-Gly-Phe-Met-NH2
  • HY-P4679
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)
    		Agonist
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist.
    (N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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