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-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-172637
    Phenethyl 4-ANPP
    		Agonist
    Phenethyl 4-ANPP is a MOR (μ-opioid receptor) agonist. Phenethyl 4-ANPP is an analytical reference standard that is structurally similar to known opioids.
    Phenethyl 4-ANPP
  • 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
  • HY-G0021R
    N-Desmethylclozapine (Standard)
    		Agonist
    N-Desmethylclozapine (Standard) is the analytical standard of N-Desmethylclozapine. This product is intended for research and analytical applications. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
    N-Desmethylclozapine (Standard)
  • HY-P1300
    [(pF)Phe4]Nociceptin(1-13)NH2
    		Agonist
    [(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).
    [(pF)Phe4]Nociceptin(1-13)NH2
  • HY-P3646
    [DAla2] Dynorphin A (1-9) (porcine)
    [DAla2] Dynorphin A (1-9) (porcine) is a dynorphin, which can be used in studies of analgesic, addiction, and depression.
    [DAla2] Dynorphin A (1-9) (porcine)
  • 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-105628A
    Prodilidine hydrochloride
    Prodilidine (CI-427) hydrochloride is a potent analgetic agent.
    Prodilidine hydrochloride
  • 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-P3547
    (D-Met2,Pro5)-Enkephalinamide
    		Agonist
    (D-Met2,Pro5)-Enkephalinamide is a highly potent opiate agonist, and shows antinociceptive activity.
    (D-Met2,Pro5)-Enkephalinamide
  • HY-W754114
    Nalmefene Sulfate-d3
    Nalmefene Sulfate-d3 is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene Sulfate-d<sub>3</sub>
  • HY-P3445
    Anrikefon
    		Agonist
    Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect.
    Anrikefon
  • HY-P2018
    FK 33-824
    		Agonist
    FK 33-824, a synthetic analogue of Met-enkephalin, is a selective agonist of the μ-opioid receptor (μ-OR).
    FK 33-824
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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