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-123142
    RX809055AX
    		Antagonist
    RX 809055AX is a potent long lasting opioid antagonist with selectivity towards at mu and delta receptors.
    RX809055AX
  • HY-A0118S1
    Naloxegol-13C,d2
    		Antagonist
    Naloxegol-13C,d2 (NKTR-118-13C,d2) is 13C labeled Naloxegol. Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
    Naloxegol-<sup>13</sup>C<sub>,d<sub>2</sub>
  • HY-100903R
    Norbinaltorphimine dihydrochloride (Standard)
    		Antagonist
    Norbinaltorphimine dihydrochloride (Standard) is the analytical standard of Norbinaltorphimine dihydrochloride (HY-100903). This product is intended for research and analytical applications. Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain.
    Norbinaltorphimine dihydrochloride (Standard)
  • HY-13243S1
    Alvimopan-d7
    		Antagonist
    Alvimopan-d7 (ADL 8-2698-d7) is deuterium labeled Alvimopan. 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-d<sub>7</sub>
  • HY-123689R
    Samidorphan (Standard)
    		Antagonist
    Samidorphan (Standard) is the analytical standard of Samidorphan. This product is intended for research and analytical applications. 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 can improve the behavior of depressed animals.
    Samidorphan (Standard)
  • HY-13274A
    JTC-801 free base
    		Antagonist
    JTC-801 free base is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2?nM.
    JTC-801 free base
  • HY-114452R
    LY2940094 (Standard)
    		Antagonist
    LY2940094 (Standard) is the analytical standard of LY2940094. This product is intended for research and analytical applications. LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
    LY2940094 (Standard)
  • HY-169822
    5′-Guanidinonaltrindole
    		Antagonist
    5′-Guanidinonaltrindole (GNTI) is a selective kappa opioid receptor antagonist.
    5′-Guanidinonaltrindole
  • HY-W778148
    O,O-Diethyl dithiophosphate-13C4 ammonium
    		Antagonist
    O,O-Diethyl dithiophosphate-13C4 ammonium is the 13C labeled isotope of O,O-Diethyl dithiophosphate ammonium.
    O,O-Diethyl dithiophosphate-<sup>13</sup>C<sub>4</sub> ammonium
  • HY-13243R
    Alvimopan (Standard)
    		Antagonist
    Alvimopan (Standard) is the analytical standard of Alvimopan. This product is intended for research and analytical applications. 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 (Standard)
  • HY-10487R
    JDTic dihydrochloride (Standard)
    		Antagonist
    JDTic dihydrochloride (Standard) is the analytical standard of JDTic dihydrochloride (HY-10487). This product is intended for research and analytical applications. JDTic dihydrochloride is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
    JDTic dihydrochloride (Standard)
  • HY-123689A
    Samidorphan hydrochloride
    		Antagonist
    Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo. Samidorphan can improve the behavior of depressed animals.
    Samidorphan hydrochloride
  • HY-107749R
    ML 190 (Standard)
    		Antagonist
    ML 190 (Standard) is the analytical standard of ML 190 (HY-107749). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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