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 (124):

Cat. No. Product Name Effect Purity
  • HY-P0210
    DAMGO Agonist 99.13%
    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-101177
    Naltrindole hydrochloride Antagonist
    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-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-B0418A
    Loperamide hydrochloride Agonist 99.79%
    Loperamide hydrochloride (R-18553 hydrochloride) 是阿片受体 (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-101718
    Aticaprant Antagonist 99.86%
    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-P1335A
    CTAP TFA Antagonist
    CTAP TFA 是一种强效、高选择性的脑渗透类阿片受体 (μ opioid receptor）拮抗剂 (IC50=3.5 nM)，对 δ opioid 受体 (IC50=4500 nM) 和生长抑素受体具有超过1200倍的选择性。CTAP TFA 可用于L -多巴胺 (HY-N0304) 诱导的运动障碍 (LID) 的研究。
  • HY-13101
    MCOPPB triHydrochloride Agonist 99.35%
    MCOPPB 3Hcl 是一种伤害感受肽受体激动剂，pKi为10.07；其他阿片受体的活性较弱。
  • HY-17609
    Difelikefalin Agonist 99.15%
    Difelikefalin (CR-845; FE-202845) 是周边限制性的，选择性的 κ 阿片受体 (KOR) 激动剂。Difelikefalin 具有抗炎作用，并在慢性肾脏病等疾病中具有调节瘙痒的潜力。
  • HY-15122A
    Sinomenine hydrochloride Activator 99.46%
    Sinomenine hydrochloride (Cucoline hydrochloride) 是来自 Sinomenium acutum 的一种生物碱，是 NF-κB 活化的阻断剂。Sinomenine 也是 μ 阿片受体 (μ-opioid receptor) 激活剂。
  • 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-12745A
    Nalfurafine hydrochloride Agonist 99.93%
    Nalfurafine hydrochloride (TRK-820 hydrochloride) 是一种强效选择性，具有口服活性的 G 蛋白偏倚 kappa opioid receptor (KOR) 激动剂，具有很高的翻译潜力。Nalfurafine hydrochloride (TRK-820 hydrochloride) 增强了 MOR 靶向镇痛药的生物学作用，它还有潜力用于尿毒症瘙痒的相关研究。
  • 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-13274
    JTC-801 Antagonist 99.75%
    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-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-101386
    PZM21 Agonist 99.57%
    PZM21 是高效选择性的 μ opioid 受体激动剂，EC50 值为 1.8 nM。
  • 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-P0288
    [Leu5]-Enkephalin Agonist 99.81%
    [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-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-15536
    Cebranopadol Agonist
    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 99.83%
    Nociceptin 是一种十七肽，为 nociceptin 受体的内源性配体，具有镇痛作用。
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