2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-17417R
    Naloxone hydrochloride (Standard) Antagonist
    Naloxone (hydrochloride) (Standard) is the analytical standard of Naloxone (hydrochloride). This product is intended for research and analytical applications. Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.
    Naloxone hydrochloride (Standard)
  • HY-156131
    Loperamide Agonist 99.85%
    Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with Ki valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE2 (HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea.
    Loperamide
  • 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-120511
    KNT-127 Agonist 99.11%
    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-101205
    ICI-199441 hydrochloride Agonist 99.30%
    ICI-199441 hydrochloride is a potent and selective κ-opioid receptor agonist with analgesic effects. ICI 199441 hydrochloride can improve heart resistance to ischemia/reperfusion.
    ICI-199441 hydrochloride
  • HY-107748
    5'-Guanidinonaltrindole hydrochloride Antagonist 98.65%
    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-101416
    Vanilpyruvic acid 98.28%
    Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid
  • HY-101231
    ICI-204448 98.09%
    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-P0098
    [D-Ala2]leucine-enkephalin Agonist 98.92%
    [D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors.
    [D-Ala2]leucine-enkephalin
  • HY-107747
    GR 89696

    GR 89696

    		Agonist 99.88%
    GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.
    GR 89696
  • HY-P1302
    Orphanin FQ(1-11) Agonist 99.83%
    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-150332
    N-Propionitrile Chlorphine hydrochloride 98.2%
    N-Propionitrile Chlorphine hydrochloride is structurally similar to known opioids.
    N-Propionitrile Chlorphine hydrochloride
  • HY-15708
    LY2795050 Antagonist 98.12%
    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-109054A
    O-Desmethyltramadol hydrochloride Agonist 99.79%
    O-Desmethyltramadol hydrochloride is the main active metabolite of tramadol (Tramadol) and can cross the blood-brain barrier. O-Desmethyltramadol hydrochloride mainly exerts its analgesic effect by activating the µ-opioid receptor (µ-OR).
    O-Desmethyltramadol hydrochloride
  • HY-100122
    Bevenopran Antagonist 99.09%
    Bevenopran is a peripheral μ-opioid receptor antagonist.
    Bevenopran
  • HY-14157
    ADL-5747 Agonist 99.82%
    ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms.
    ADL-5747
  • 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-P1742
    Gluten Exorphin B5 Agonist 98.23%
    Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats.
    Gluten Exorphin B5
  • HY-12392
    Iprindole Agonist 99.55%
    Iprindole, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole induces lamellar body formation but devoid of lamellar bodies. Iprindole can be used for the research of depression.
    Iprindole
  • 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
製品番号 製品名 / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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