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-159088
    KOR agonist 2
    		Agonist
    KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes.
    KOR agonist 2
  • HY-112692A
    AT-121 hydrochloride
    		Agonist
    AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.
    AT-121 hydrochloride
  • HY-W725190A
    Piperidylthiambutene
    		Agonist
    Piperidylthiambutene is a potent µ-opioid receptor (MOR) agonist with a Ki of 2.75 nM. Piperidylthiambutene exhibits analgesic and antitussive properties and can be utilized in relevant research.
    Piperidylthiambutene
  • HY-P3043
    Bilaid A
    		Agonist
    Bilaid A is a μ-opioid receptor agonist that can be extracted from Penicillium. The Ki value is 3.1 μM. Bilaid A can be used in pain research.
    Bilaid A
  • HY-107094A
    MT-7716 free base
    		Agonist
    MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention.
    MT-7716 free base
  • HY-P3839
    Nocistatin
    		Agonist
    Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia.
    Nocistatin
  • HY-186105A
    (-)-P7C3-S243
    		Inhibitor
    (-)-P7C3-S243 is an orally active, blood-brain barrier permeable neuroprotective agent. (-)-P7C3-S243 binds to μ-opioid Receptor and TSPO. (-)-P7C3-S243 inhibits the premature apoptosis death of newborn hippocampal neurons, protects mature nigral dopaminergic neurons, promotes neuronal survival and prevents cognitive impairment. (-)-P7C3-S243 ameliorates depression-like behaviors in rat models. (-)-P7C3-S243 is applicable to research related to Parkinson's disease and Alzheimer's disease.
    (-)-P7C3-S243
  • HY-P1246
    Neuropeptide AF (human)
    		Inhibitor
    Neuropeptide AF (human) is an endogenous antiopioid peptide.
    Neuropeptide AF (human)
  • HY-163917
    SalA-VS-08
    		Agonist
    SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia.
    SalA-VS-08
  • HY-178235
    MDAN-21
    MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia.
    MDAN-21
  • HY-106131
    RSD-921
    		Agonist
    RSD-921 (PD-123497) is a potent Na+ channel blocker with anti-arrhythmic activity. RSD-921 displays a low affinity for κ-opioid receptors and behaves as a weak κ-agonist in vitro. RSD 921 displays state-, time- and voltage-dependent block of the open state of cardiac, skeletal muscle and neuronal Na+ channels expressed in Xenopus oocytes. RSD-921 can be used for cardiac arrhythmias research.
    RSD-921
  • HY-P1319
    Nociceptin(1-7)
    		Agonist
    Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
    Nociceptin(1-7)
  • HY-105682
    Alimadol
    		Agonist
    Alimadol is an orally active opioid receptor agonist with analgesic activity. Alimadol can be used for the research of pain.
    Alimadol
  • HY-W019878
    β-Endorphin, rat
    β-Endorphin, rat (β-Lipotropin 61-91), a neuropeptide, is involved in cardiovascular regulation. β-Endorphin, rat induces marked, prolonged muscular rigidity and immobility similar to a catatonic state in rats.
    β-Endorphin, rat
  • 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-121854A
    Bromadoline maleate
    		Activator
    Bromadoline maleate is an opioid analgesic selective for the μ-opioid receptor, exhibiting analgesic activity in various biological fluids. Bromadoline maleate has been successfully quantified alongside its N-demethylated metabolites in human and canine samples.
    Bromadoline maleate
  • HY-N12180A
    Hodgkinsine
    		Agonist
    Hodgkinsine is an opioid receptor agonist and NMDA receptor antagonist, which has analgesic and anti-injurial effects. In addition, Hodgkinsine has antiviral, antibacterial and antifungal activities.
    Hodgkinsine
  • HY-109064
    Loxicodegol
    		Agonist
    Loxicodegol (Oxycodegol) is a first-in-class, long-acting, orally active, and selective mu-opioid agonist with structural properties that reduce its rate of entry across the blood-brain barrier compared with traditional mu-opioid agonists.
    Loxicodegol
  • HY-159923
    BPRMU191
    		Modulator
    BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation.
    BPRMU191
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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