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-167946
    CP-866087
    		Antagonist
    CP-866087 is a new, highly effective, and selective antagonist of the mu-opioid receptor designed for exploring female sexual dysfunction.
    CP-866087
  • HY-B1485
    Nalmefene hydrochloride
    		Antagonist 99.19%
    Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence.
    Nalmefene hydrochloride
  • HY-13222A
    BAN ORL 24 free base
    		Antagonist
    BAN ORL 24 free base is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 free base has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 free base can be used for the research of cancer and analgesic.
    BAN ORL 24 free base
  • HY-107745
    SDM25N hydrochloride
    		Antagonist
    SDM25N hydrochloride, a δ-opioid receptor antagonist, is a potent DENV inhibitor. SDM25N hydrochloride targets the viral NS4B protein and restricts genomic RNA replication.
    SDM25N hydrochloride
  • HY-144607
    Mu opioid receptor antagonist 2
    		Antagonist
    Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD).
    Mu opioid receptor antagonist 2
  • HY-129422
    Diallyl G
    		Antagonist
    Diallyl G is a delta-opioid receptor antagonist. Diallyl G shows inhibitory effect on GTPase.
    Diallyl G
  • HY-19902
    GSK1521498
    		Antagonist
    GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498
  • HY-135698
    Methocinnamox
    		Antagonist
    Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction.
    Methocinnamox
  • HY-179282
    Mu opioid receptor antagonist 9
    		Antagonist
    Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD).
    Mu opioid receptor antagonist 9
  • HY-11052A
    Trap-101 hydrochloride
    		Antagonist
    Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
    Trap-101 hydrochloride
  • HY-P5756
    CSD-CH2(1,8)-NH2
    		Antagonist
    CSD-CH2(1,8)-NH2 is a selective and competitive KOR antagonist (Ki: 6.8 nM). CSD-CH2(1,8)-NH2 inhibits calcium mobilization in DRG neurons. CH2(1,8)-NH2 antagonizes the antinociceptive effect of U50,488. CSD-CH2(1,8)-NH2 can be used for research of neuropsychiatric disorders.
    CSD-CH2(1,8)-NH2
  • HY-137180
    Naloxonazine
    		Antagonist
    Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function.
    Naloxonazine
  • HY-115844
    LY-99335
    		Antagonist
    LY-99335 is an anesthetic antagonist with behavioral inhibitory activity. LY-99335 exhibits large dose separation at specific doses, indicating its potential in anesthetic antagonism.
    LY-99335
  • HY-17417AR
    Naloxone (Standard)
    		Antagonist
    Naloxone (Standard) is the analytical standard of Naloxone. This product is intended for research and analytical applications. Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.
    Naloxone (Standard)
  • HY-174422
    Opioid receptor antagonist 2
    		Antagonist
    Opioid receptor antagonist 2 (Compound 9) is a potent opioid receptor antagonist. Opioid receptor antagonist 2 can reverse ventilatory depression and vocal cord closure induced by fentanyl analogs in mice. Opioid receptor antagonist 2 is promising for research of acute poisoning such as respiratory depression caused by overdose of opioids.
    Opioid receptor antagonist 2
  • HY-181605
    MOR antagonist 2 hydrochloride
    		Antagonist
    MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder.
    MOR antagonist 2 hydrochloride
  • HY-149386
    D3R/MOR antagonist 1
    		Antagonist
    D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism.
    D3R/MOR antagonist 1
  • HY-155320
    Mu opioid receptor antagonist 7
    		Antagonist
    Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder.
    Mu opioid receptor antagonist 7
  • HY-101199
    N-Benzylnaltrindole hydrochloride
    		Antagonist
    N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function.
    N-Benzylnaltrindole hydrochloride
  • HY-107750A
    Cyprodime hydrochloride
    		Antagonist
    Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect.
    Cyprodime hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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