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-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-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 99.40%
    Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects.
    Trimebutine
  • HY-120511
    KNT-127
    		Agonist 99.60%
    KNT-127 is a potent δ-opioid receptor agonist that crosses the blood-brain barrier (BBB). 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 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 has analgesic, antidepressant and antianxiety activities.
    KNT-127
  • 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-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-123689
    Samidorphan
    		Antagonist 99.04%
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.
    Samidorphan
  • HY-123689
    Samidorphan
    		Modulator 99.04%
    Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.
    Samidorphan
  • HY-107744
    Nalmefene
    		Antagonist 99.70%
    Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence.
    Nalmefene
  • HY-107094
    MT-7716 hydrochloride
    		Agonist 99.06%
    MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
    MT-7716 hydrochloride
  • 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-15708
    LY2795050
    		Antagonist 98.68%
    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-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-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-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-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-164747
    Isotodesnitazene
    		Agonist 99.78%
    Isotodesnitazene is a kind of opioids. Isotodesnitazene primarily acts on μ-opioid receptors (MOR). Isotodesnitazene has an EC50 of 34.8 nM for MOR-βarr2 and 142 nM for MOR-mini-Gi. Isotodesnitazene can be used in the study of opioids.
    Isotodesnitazene
  • 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-120949
    (1R,2R)-U-50488 hydrochloride
    		Agonist 99.14%
    (1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (1R,2R)-U-50488 hydrochloride
  • HY-101317
    TAN-67 dihydrobromide
    		Agonist 99.20%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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