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-141515
    BMS-986121
    		Modulator 98.89%
    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-100122
    Bevenopran
    		Antagonist 99.82%
    Bevenopran is a peripheral μ-opioid receptor antagonist.
    Bevenopran
  • HY-101231
    ICI-204448
    		98.68%
    ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guinea pig cerebellum membranes.
    ICI-204448
  • HY-107384A
    Asimadoline hydrochloride
    		Agonist 99.82%
    Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).
    Asimadoline hydrochloride
  • HY-P1866A
    β-Endorphin, equine TFA
    		Agonist
    β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. β-Endorphin, equine TFA has analgesic properties.
    β-Endorphin, equine TFA
  • HY-134189A
    EST73502 monohydrochloride
    		Agonist 99.58%
    EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.
    EST73502 monohydrochloride
  • 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-P1317A
    Nociceptin (1-13), amide TFA
    		Agonist 99.67%
    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-101079
    BRL 52537 hydrochloride
    		Agonist 98.14%
    BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage.
    BRL 52537 hydrochloride
  • 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-107722
    SCH 221510
    		Agonist 99.00%
    SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect.
    SCH 221510
  • HY-P3609
    CR 665
    		Agonist 99.65%
    CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain.
    CR 665
  • HY-P1170
    N-terminally acetylated Leu-enkephalin
    		Agonist 99.49%
    N-terminally acetylated Leu-enkephalin is the N-terminally acetylated form of Leu-enkephalin. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
    N-terminally acetylated Leu-enkephalin
  • HY-15997C
    (±)-U-50488 hydrate hydrochloride
    		Agonist
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (±)-U-50488 hydrate hydrochloride
  • HY-101317
    TAN-67 dihydrobromide
    		Agonist ≥99.0%
    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-B0418AS
    Loperamide-d6 hydrochloride
    		Agonist 99.07%
    Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
    Loperamide-d<sub>6</sub> hydrochloride
  • HY-19627
    Naldemedine
    		Antagonist
    Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
    Naldemedine
  • HY-P0318
    Hemorphin-7
    		Activator
    Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
    Hemorphin-7
  • HY-P1334A
    DPDPE TFA
    		Agonist 99.94%
    DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.
    DPDPE TFA
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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