T8414
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Opioid Receptor
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SNC 80 (NIH 10815) 是有效的,高度选择性的非肽类 δ 阿片 (δ-opioid) 受体激动剂,Ki 为1.78 nM,IC50 为 2.73 nM。SNC80 还以 EC50 为 52.8 nM 来选择性激活 HEK293 细胞中的 μ-δ 异聚体。SNC80 具有抗伤害性,抗痛觉过敏和抗抑郁样作用,并可用于多种头痛症的研究。 |
T37610
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Opioid Receptor
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AT-121 是一种双重μ-阿片和神经肽受体部分激动剂(Kis 分别为 16.49 和 3.67 nM)。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合(EC50s 分别为 19.6 和 34.7 nM)。AT-121(0.003-0.03 mg/kg)能以剂量依赖的方式降低辣椒素诱导的热异感,但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中,AT-121 每次注射剂量为 0.3 至 10 μg/kg,它缺乏强化作用(一种潜在的滥用标志),不能减少食物颗粒的强化作用。AT-121(0.01 或 0.03 毫克/千克)不会诱发恒河猴的超痛觉,超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药,具有抗伤害和止痛作用。 |
T27253
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Elismetrep is a non-opioid analgesic. |
T23972
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DDD-028 is a potential non-opioid and non-cannabinoid analgesic. It was used for treating neuropathic and inflammatory pain. |
T34784
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TAN67 is the first effective selective non-peptide delta1 opioid receptor. |
T31631
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Enkephalin-leu, ala(2)-ser(6)- is an active compound at the delta (non-complexed) opioid receptor. |
T25690
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Levallorphan tartrate is an opioid antagonist with properties similar to those of NALOXONE. Levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid ce |
T70503
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Exp 631 is a centrally-acting non-opioid analgesic; exhibits serotonin and norepinephrine reuptake inhibiting activities. |
T26475
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A-286501 is an orally active adenosine kinase inhibitor (IC50=0.47 nM). A-286501 effectively attenuates nociception by a non-opioid, non-non-steroidal anti-inflammatory drug ADO, receptor mediated mechanism. |
T23313
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Others
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non-peptide δ1 opioid receptor agonist |