2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • 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-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-P0186A
    Endomorphin 2 TFA
    		Agonist 99.04%
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2 TFA
  • 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-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-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-150332
    N-Propionitrile Chlorphine hydrochloride
    		98.6%
    N-Propionitrile Chlorphine hydrochloride is structurally similar to known opioids.
    N-Propionitrile Chlorphine hydrochloride
  • 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-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-N2571
    Corydine
    		Agonist 99.93%
    Corydine is a HIV-1 reverse transcriptase inhibitor and μ-opioid receptor (MOR) agonist, with an IC50 of 356.7 μg/mL against HIV-1 reverse transcriptase, an EC50 of 0.51 μM for MOR, and a Ki of 2.82 μM for MOR. Corydine produces antinociceptive effects by inhibiting acetic acid-induced writhing behavior in a MOR-dependent manner. Corydine inhibits the proliferation of cancer cells, mitogen-stimulated lymphocytes and IL-2-dependent cells. Corydine can be used in studies related to human immunodeficiency virus infection, visceral pain, leukemia, melanoma, bladder cancer and colon adenocarcinoma.
    Corydine
  • HY-100122
    Bevenopran
    		Antagonist 99.09%
    Bevenopran is a peripheral μ-opioid receptor antagonist.
    Bevenopran
  • 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-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 99.68%
    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-136832
    Noribogaine hydrochloride
    		Modulator 99.90%
    Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC50=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity.
    Noribogaine 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-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
Art. -Nr. Produktname / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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