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-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-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-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-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
  • HY-19267
    Ro-48-6791
    		Activator
    Ro-48-6791 is a compound that may have the activity of activating opioid receptors. Computational studies have found that it may bind to and activate opioid receptors, and may mediate or increase their related physiological effects and side effects.
    Ro-48-6791
  • 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-P1333A
    Dynorphin A TFA
    		Agonist
    Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease.
    Dynorphin A TFA
  • HY-18617
    rel-SB-612111 hydrochloride
    		Inhibitor
    rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.
    rel-SB-612111 hydrochloride
  • HY-163277
    PIPE-3297
    		Agonist
    PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity.
    PIPE-3297
  • HY-P3546
    [DPen2, Pen5] Enkephalin
    		Agonist
    [DPen2, Pen5] Enkephalin is a δ-opioid receptor selective analog of [Leu5]-Enkephalin (HY-P0288).
    [DPen2, Pen5] Enkephalin
  • HY-129422
    Diallyl G
    		Antagonist
    Diallyl G is a delta-opioid receptor antagonist. Diallyl G shows inhibitory effect on GTPase.
    Diallyl G
  • HY-121800
    ML138
    		Agonist
    ML138, a κ opioid receptor agonist, is a MLPCN probe.
    ML138
  • HY-P1318
    Ac-RYYRIK-NH2
    		Agonist
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
    Ac-RYYRIK-NH2
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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