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-101392
    Harmane
    		Inhibitor 99.91%
    Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .
    Harmane
  • HY-19627A
    Naldemedine tosylate
    		Antagonist
    Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine tosylate is predicted to bind to 3CLpro encoded by SARS-CoV2 genome.
    Naldemedine tosylate
  • HY-Y0790
    Cuminaldehyde
    		Inhibitor 99.03%
    Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL), α-glucosidase (IC50=0.5 mg/mL) and lipoxygenase (IC50=1370 μM). Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases.
    Cuminaldehyde
  • HY-12363
    U-69593
    		Agonist 99.73%
    U-69593 is a potent and selective κ1-opioid receptor agonist. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum.
    U-69593
  • HY-P2159
    Dynorphin A (1-8)
    		99.88%
    Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
    Dynorphin A (1-8)
  • HY-P1329A
    CTOP TFA
    		Antagonist 99.84%
    CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity.
    CTOP TFA
  • HY-105343
    BW-180C
    		Agonist 99.92%
    BW-180C ([D-Ala2, D-Leu5]-Enkephalin; DADLE) is an δ opioid receptor (DOR) agonist, which belongs to the enkephalin family. Neuroprotective agent. BW-180C reversibly inhibits cellular transcription in neurons without causing cell injury.
    BW-180C
  • HY-P0088
    Porcine dynorphin A(1-13)
    		Agonist 99.81%
    Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.
    Porcine dynorphin A(1-13)
  • HY-137279
    Naloxone methiodide
    		Antagonist 99.7%
    Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier.
    Naloxone methiodide
  • HY-P1087
    Adrenorphin
    		Agonist
    Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
    Adrenorphin
  • HY-P0210B
    DAMGO TFA
    		Agonist 99.60%
    DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR.
    DAMGO TFA
  • HY-P1013A
    Deltorphin 2 TFA
    		Agonist 99.88%
    Deltorphin 2 TFA is a selective peptide agonist for the δ opioid receptor.
    Deltorphin 2 TFA
  • HY-13222
    BAN ORL 24
    		Antagonist 99.68%
    BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with KI value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic.
    BAN ORL 24
  • HY-111454
    SR17018
    		Agonist 98.01%
    SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.
    SR17018
  • HY-101416
    Vanilpyruvic acid
    		98.28%
    Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid
  • HY-139690
    CCG258747
    		Inhibitor 99.17%
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
    CCG258747
  • HY-P1594A
    Dynorphin A (1-10) (TFA)
    		Agonist 98.19%
    Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC50 of 42.0 μM.
    Dynorphin A (1-10) (TFA)
  • HY-115066
    GSK1521498 free base
    		Antagonist 98.55%
    GSK1521498 free base is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents.
    GSK1521498 free base
  • HY-120949
    (1R,2R)-U-50488 hydrochloride
    		Agonist 99.14%
    (1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (1R,2R)-U-50488 hydrochloride
  • HY-128865
    BPR1M97
    		Agonist 98.32%
    BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.
    BPR1M97
Cat. No. Product Name / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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