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-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-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-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-P3445A
    Anrikefon acetate
    		Agonist 99.25%
    Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect.
    Anrikefon acetate
  • 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-13716A
    Noscapine hydrochloride
    		Agonist 99.87%
    Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
    Noscapine hydrochloride
  • 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-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-P1170
    N-terminally acetylated Leu-enkephalin
    		Agonist 99.49%
    N-terminally acetylated Leu-enkephalin is the N-terminally acetylated form of Leu-enkephalin. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
    N-terminally acetylated Leu-enkephalin
  • HY-118949
    LY255582
    		Antagonist ≥98.0%
    LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity.
    LY255582
  • HY-113316A
    (±)-Salsolinol hydrochloride
    		Agonist 98%
    (±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA).
    (±)-Salsolinol hydrochloride
  • HY-P1334A
    DPDPE TFA
    		Agonist 99.81%
    DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.
    DPDPE TFA
  • HY-101231
    ICI-204448
    		98.68%
    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-126941
    Hecogenin acetate
    		98.57%
    Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
    Hecogenin acetate
  • 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-101223
    DIPPA hydrochloride
    		Antagonist 99.7%
    DIPPA hydrochloride is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA hydrochloride can be used for the research of anxiety and antidepressant.
    DIPPA hydrochloride
  • HY-P1317A
    Nociceptin (1-13), amide TFA
    		Agonist 99.67%
    Nociceptin (1-13), amide TFA is a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.
    Nociceptin (1-13), amide TFA
  • HY-107749
    ML 190
    		Antagonist 98.2%
    ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively.
    ML 190
  • HY-P1013
    Deltorphin 2
    		Agonist
    Deltorphin 2 is a selective peptide agonist for the δ opioid receptor.
    Deltorphin 2
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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