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-128865
    BPR1M97
    		Agonist 98.32%
    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-13044
    ADL-5859 hydrochloride
    		Agonist 99.77%
    ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
    ADL-5859 hydrochloride
  • HY-13101
    MCOPPB trihydrochloride
    		Agonist 99.98%
    MCOPPB trihydrochloride is a nociceptin receptor agonist with pKi of 10.
    MCOPPB trihydrochloride
  • 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.
    UFP-101 TFA
  • HY-104006
    CYM51010
    		Agonist 99.12%
    CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms.
    CYM51010
  • HY-N0398
    Sec-O-Glucosylhamaudol
    		Inhibitor 99.81%
    Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.
    Sec-O-Glucosylhamaudol
  • HY-115066
    GSK1521498 free base
    		Antagonist 98.55%
    GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498 free base
  • HY-111454
    SR17018
    		Agonist 98.01%
    SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
    SR17018
  • HY-107741
    SNC162
    		Agonist 99.72%
    SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like and antinociceptiv effects.
    SNC162
  • HY-124959
    Spiradoline mesylate
    		Agonist 99.95%
    Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guinea pig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier.
    Spiradoline mesylate
  • HY-P1087
    Adrenorphin
    		Agonist
    Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
    Adrenorphin
  • HY-114072
    J-113397
    		Antagonist 99.00%
    J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.
    J-113397
  • HY-P1337
    Dynorphin B (1-13)
    		Agonist 98.09%
    Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
    Dynorphin B (1-13)
  • HY-101376
    (+)-N-Allylnormetazocine hydrochloride
    		Antagonist ≥99.0%
    (+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.
    (+)-N-Allylnormetazocine hydrochloride
  • HY-107721
    (±)-J-113397
    		Antagonist 98.59%
    (±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.
    (±)-J-113397
  • HY-P3870A
    DALDA acetate
    		Agonist 99.53%
    DALDA acetate is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects.
    DALDA acetate
  • HY-107747
    GR 89696
    		Agonist 99.88%
    GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.
    GR 89696
  • 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-117040
    nor-Binaltorphimine
    		Antagonist 98.70%
    nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo.
    nor-Binaltorphimine
  • HY-B0418AR
    Loperamide (hydrochloride) (Standard)
    		Agonist 99.89%
    Loperamide (hydrochloride) (Standard) is the analytical standard of Loperamide (hydrochloride). This product is intended for research and analytical applications. 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.
    Loperamide (hydrochloride) (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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