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 相关产品 (87):

Cat. No. Product Name Effect Purity
  • HY-P0210
    DAMGO Agonist 98.10%
    DAMGO 是 一种选择性的 μ-阿片受体 (μ-OPR) 激动剂，Kd 值为 3.46 nM。
  • HY-12745A
    Nalfurafine hydrochloride Agonist 99.93%
    Nalfurafine hydrochloride是一种κ-opioid激动剂，是日本批准的抗瘙痒药物。
  • HY-101386
    PZM21 Agonist 99.45%
    PZM21是高效选择性的μ opioid receptor受体激动剂，EC50值为1.8 nM。
  • HY-B0418A
    Loperamide hydrochloride Agonist 99.69%
    Loperamide hydrochloride (R-18553 hydrochloride) 是用于治疗腹泻的阿片受体 (opioid receptor) 激动剂。Loperamide hydrochloride 也是一种选择性的竞争性人类肠道羧酸酯酶 (hiCE) 抑制剂。Loperamide hydrochloride 具有止泻作用。
  • HY-101177
    Naltrindole hydrochloride Antagonist 99.68%
    Naltrindole hydrochloride是高效，选择性的非多肽类 δ opioid 受体拮抗剂，Ki值为0.02 nM。
  • HY-124754
    BTRX-335140 Inhibitor
    BTRX-335140 (CYM-53093) 是一种有效且选择性的口服 κ opioid receptor (KOR) 拮抗剂，对 κOR，μOR 和 δOR 具有拮抗剂活性，IC50 值分别为 0.8 nM，110 nM 和 6500 nM。BTRX-335140 在大鼠中具有良好的体外 ADMET 和体内药代动力学特征。BTRX-335140 可以很好地分布到 CNS 中。 ADMET (吸收，分布，代谢，排泄和毒性)。
  • HY-P1467A
    [Met5]-Enkephalin, amide TFA Agonist 99.71%
    [Met5]-Enkephalin, amide TFA 是一种 δ 和 ζ 阿片受体 (opioid receptor) 激动剂。
  • HY-N0164
    Matrine Agonist >98.0%
    Matrine (Matridin-15-one) 是来源于植物的生物碱，有抗肿瘤活性，是kappa阿片受体激动剂。
  • HY-10487
    JDTic dihydrochloride Antagonist 99.79%
    JDTic dihydrochloride 是一种有效的 kappa-opioid receptors (KOR) 的拮抗剂，常用于神经系统疾病的研究。
  • HY-G0021
    N-Desmethylclozapine Agonist 99.72%
    N-Desmethylclozapine 是非典型抗精神病药 Clozapine 的主要活性代谢产物。N-Desmethylclozapine 是一种有效的、变构的部分 M1 受体激动剂 (EC50=115 nM)，能通过 M1 受体激活增强海马 N-methyl-d-aspartate (NMDA) 受体电流。N-Desmethylclozapine 也是 δ-opioid 激动剂。
  • HY-13044
    ADL-5859 Agonist 99.77%
    ADL5859是δ-阿片受体选择性激动剂，Ki为0.8 nM，对hERG有弱抑制性。
  • HY-15122A
    Sinomenine hydrochloride Activator >98.0%
    Sinomenine hydrochloride 是 NF-κB 活化的阻断剂，也是 μ 阿片受体 (μ-opioid receptor) 的激活剂。
  • HY-101718
    Aticaprant Antagonist 99.24%
    Aticaprant (CERC-501) 是一种有效地可渗透中枢神经的kappa opioid受体拮抗剂，Ki值为0.807 nM。
  • HY-16655A
    Oliceridine hydrochloride Agonist 99.78%
    Oliceridine hydrochloride (TRV130 hydrochloride) 是新颖的 MOR 激动剂，能够优先激活 G-protein 信号通路，而对 β-arrestin 的作用稍弱。
  • HY-P0288
    [Leu5]-Enkephalin Agonist 99.72%
    [Leu5]-Enkephalin 是一种具有吗啡药性的五肽。作为阿片受体 (opioid receptors) 激动剂。
  • HY-13274
    JTC-801 Antagonist 99.73%
    JTC-801 是一种具有选择性的 opioid receptor-like1 (ORL1) receptor 抑制剂，其 Ki 值为 8.2 nM。
  • HY-15536
    Cebranopadol Agonist 98.76%
    Cebranopadol 是NOP 和 opioid receptor 激动剂，作用于人NOP，MOP，KOP 和δ-阿片肽(DOP)受体，Ki/EC50 分别为 0.9 nM/13 nM，0.7 nM/1.2 nM，2.6 nM/17 nM，18 nM/110 nM。
  • HY-P0183
    Nociceptin Agonist 99.79%
    Nociceptin 是一种十七肽，为 nociceptin 受体的内源性配体，具有镇痛作用。
  • HY-P0073
    Tyr-Gly-Gly-Phe-Met-OH Activator 99.81%
    Tyr-Gly-Gly-Phe-Met-OH 通过结合阿片样物质受体 (opioid receptor)，可调控人类免疫功能，抑制肿瘤生长。
  • HY-13222
    BAN ORL 24 Antagonist
    BAN ORL 24是NOP受体拮抗剂，对NOP，κ-，μ-和δ-受体的IC50分别为0.27，2500，6700和> 10000 nM。
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