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-13243
    Alvimopan
    		Antagonist 98.66%
    Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.
    Alvimopan
  • HY-B0380
    Trimebutine
    		Agonist 99.42%
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine
  • HY-107744
    Nalmefene
    		Modulator 99.70%
    Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene
  • 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-101205
    ICI 199441
    		Agonist 99.39%
    ICI 199441 is a potent and selective κ-opioid receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion.
    ICI 199441
  • 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-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-107747
    GR 89696
    		Agonist 99.88%
    GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.
    GR 89696
  • HY-101011
    Naloxonazine dihydrochloride
    		Antagonist 98.1%
    Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity.
    Naloxonazine dihydrochloride
  • HY-P1337A
    Dynorphin B (1-13) TFA
    		Agonist
    Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor.
    Dynorphin B (1-13) TFA
  • 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-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-120511
    KNT-127
    		Agonist 99.60%
    KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (Ki = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases.
    KNT-127
  • HY-107748
    5'-Guanidinonaltrindole hydrochloride
    		Antagonist 98.72%
    5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor.
    5'-Guanidinonaltrindole hydrochloride
  • HY-P1470
    [Leu5]-Enkephalin, amide
    		Agonist
    [Leu5]-Enkephalin, amide is a δ opioid receptor agonist.
    [Leu5]-Enkephalin, amide
  • HY-101230
    ICI 174864
    		99.97%
    ICI 174864 is a highly selective, potent δ-receptor antagonist. ICI 174864 is equipotent with naloxone and can not reverse the effect of the μ-agonist [D-Ala2, MePhe4, Gly-Ol5]enkephalin or the κ-agonist-tifluadom.
    ICI 174864
  • HY-P0098
    [D-Ala2]leucine-enkephalin
    		Agonist 98.64%
    [D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin.
    [D-Ala2]leucine-enkephalin
  • HY-P1302
    Orphanin FQ(1-11)
    		Agonist 99.52%
    Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.
    Orphanin FQ(1-11)
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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