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-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-109166
    Amdakefalin
    		Agonist
    Amdakefalin is a μ and δ opioid receptors agonist with analgesic effects.
    Amdakefalin
  • 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-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-180212A
    SYK-1106 dihydrochloride
    		Agonist
    SYK-1106 dihydrochloride is a selective δ opioid receptor (DOR) agonist with an EC50 of 0.089 nM. SYK-1106 dihydrochloride shows high selectivity over MOR and KOR. SYK-1106 dihydrochloride exhibits antidepressant-like effects in the mouse forced-swimming tests. SYK-1106 dihydrochloride can be used for the research of depression.
    SYK-1106 dihydrochloride
  • 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-182563
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide
    		Ligand
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide is a μ/δ opioid receptor ligand with high μ opioid receptor selectivity and agonist activity. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide has an IC50 of 237 nM for μ receptors and 1050 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide shows Ki values of 17 nM for μ receptors and 480 nM for δ receptors. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide inhibits electrically evoked contractions of guinea pig ileum and mouse vas deferens. Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide serves as a starting compound for structure-activity relationship investigations of μ receptor recognition.
    Tyr-Ala-N-(1,3-dimethylbutyl)glycinamide
  • 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-W856819
    Eseroline
    		Agonist
    Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease.
    Eseroline
  • 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
  • HY-P3632
    [DAla2, DArg6] Dynorphin A, (1-13) (porcine)
    [DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD) is an opioid peptide (dynorphinl-13, DYN) derivative found in porcine pituitary extracts. DYN is highly potent at the peripheral opioid receptors GPI and MVD, but is readily and rapidly degraded in vivo. [DAla2, DArg6] Dynorphin A, (1-13) (porcine) has some resistance to enzymatic cleavage and prevents peptide cleavage by enzymes.
    [DAla2, DArg6] Dynorphin A, (1-13) (porcine)
  • 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-173016
    HINT1-IN-1
    		Modulator
    HINT1-IN-1 (Compound 8) is the inhibitor for histidine triad nucleotide-binding protein 1 (HINT1) with a Ki of 1.14 μM. HINT1-IN-1 affects the cross-regulation between μ-opioid receptor (MOR) and NMDA receptor (NMDAR). HINT1-IN-1 enhances the analgesic effect of morphine without causing opioid tolerance and has independent analgesic effects in mouse model.
    HINT1-IN-1
  • HY-161539
    KOR agonist 1
    		Agonist
    KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg).
    KOR agonist 1
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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