2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-P1467A
    [Met5]-Enkephalin, amide TFA Agonist 99.58%
    [Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ (zeta) opioid receptors.
    [Met5]-Enkephalin, amide TFA
  • HY-N2392
    Kukoamine A

    Kukoamine A

    		Activator 99.88%
    Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE2, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease.
    Kukoamine A
  • HY-P0088
    Porcine dynorphin A(1-13)

    Porcine dynorphin A(1-13)

    		Agonist 99.86%
    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-13044
    ADL-5859 hydrochloride Agonist 98.96%
    ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
    ADL-5859 hydrochloride
  • HY-P1335A
    CTAP TFA Antagonist 99.60%
    CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.
    CTAP TFA
  • HY-120645
    BMS-986122

    BMS-986122

    		Agonist 99.90%
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes.
    BMS-986122
  • HY-111664
    (R)-(+)-Citronellal

    (+)-Citronellal

    		Activator 98.72%
    (R)-(+)-Citronellal ((+)-Citronellal) is a monoterpenoid compound and is one of the main components of essential oils from plants such as lemon grass. (R)-(+)-Citronellal has antibacterial, antifungal, and insecticidal activities. (R)-(+)-Citronellal alleviates the bitterness of caffeine by antagonizing the bitter taste receptors Tas2r43 (IC50 = 84 μM) and Tas2R46. (R)-(+)-Citronellal generates analgesic activity by activating the opioid receptor (broad-spectrum opioid receptor) pathway, and its effect is particularly significant for inflammatory pain.
    (R)-(+)-Citronellal
  • HY-13243
    Alvimopan Antagonist 98.42%
    Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.
    Alvimopan
  • HY-114452
    LY2940094 Antagonist 99.17%
    LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.
    LY2940094
  • HY-P0244
    Dermorphin Agonist 99.36%
    Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
    Dermorphin
  • HY-107744
    Nalmefene Modulator 99.94%
    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
  • HY-137279
    Naloxone methiodide

    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-P2159
    Dynorphin A (1-8) 99.88%
    Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke.
    Dynorphin A (1-8)
  • HY-G0021
    N-Desmethylclozapine

    N-Desmethylclozapine

    		Agonist 99.10%
    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
  • HY-P1336
    Deltorphin I Agonist
    Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
    Deltorphin I
  • HY-113316A
    (±)-Salsolinol hydrochloride Agonist 98%
    (±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA).
    (±)-Salsolinol hydrochloride
  • HY-101318
    β-Funaltrexamine hydrochloride Antagonist 99.07%
    β-Funaltrexamine (β-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.
    β-Funaltrexamine hydrochloride
  • HY-P1594A
    Dynorphin A (1-10) TFA Agonist 98.64%
    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-B0188
    Mianserin Activator 99.42%
    Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.
    Mianserin
  • HY-15997B
    (±)-U-50488 hydrochloride Agonist 99.73%
    (±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist.
    (±)-U-50488 hydrochloride
製品番号 製品名 / Synonyms Application Reactivity
Opioid Receptor Isoform Comparison

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