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-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-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
  • 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-101416R
    Vanilpyruvic acid (Standard)
    Vanilpyruvic acid (Standard) is the analytical standard of Vanilpyruvic acid. This product is intended for research and analytical applications. Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid (Standard)
  • HY-P10203
    μ/κ/δ opioid receptor agonist 1
    		Agonist
    μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test.
    μ/κ/δ opioid receptor agonist 1
  • HY-P2579
    Dafphedyn
    		Agonist
    Dafphedyn is an analogue of Dynorphin (1-13). Dafphedyn has diuretic and profound analgesia effects that can be antagonized by centrally administered Naltrexone (HY-76711) or Naloxone (HY-17417A).
    Dafphedyn
  • HY-101318
    β-Funaltrexamine hydrochloride
    		Antagonist
    β-Funaltrexamine (β-FNA) hydrochloride is a selective μ opioid receptor antagonist. β-Funaltrexamine hydrochloride also inhibits cytokine-induced iNOS activation. β-Funaltrexamine hydrochloride inhibits neuroinflammation and ameliorated neuronal degeneration. β-Funaltrexamine hydrochloride has anti-inflammatory and neuroprotective effects and can be used for research of neurodegenerative diseases (eg: stroke)[1][2]
    β-Funaltrexamine hydrochloride
  • HY-106234
    ZP 120C
    		Agonist
    ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia.
    ZP 120C
  • 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-N0164R
    Matrine (Standard)
    		Agonist
    Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
    Matrine (Standard)
  • HY-170033
    3-Carboxamidonaltrexone
    3-Carboxamidonaltrexone (example 32) is a opioid receptor binding compound with Ki values of 1.9 nM, 110 nM, and 22 nM for μ-opioid receptor, δ-opioid receptor, and K-opioid receptor, respectively.
    3-Carboxamidonaltrexone
  • HY-163669
    ITI-333
    		Agonist
    ITI-333 is a tetracyclic compound with oral bioavailability and analgesic activity, targeting multiple receptors. ITI-333 can be used for research on various forms of pain.
    ITI-333
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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