哌替啶施加受体激动剂活性的α肾上腺素受体亚型(2 b)。

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高田K,克拉克DJ,戴维斯MF,吨PH值,Krause TK, Bertaccini E,迷宫

哌替啶施加受体激动剂活性的α肾上腺素受体亚型(2 b)。

麻醉学。2002年6月,96 (6):1420 - 6。

PubMed ID

12170055 (在PubMed

]

文摘

背景:阿片受体激动剂哌替啶的行为,如antishivering明显多于其他阿片类受体激动剂和非选择性阿片拮抗剂不阻塞。α受体激动剂(2)肾上腺素能受体,如可乐定、antishivering非常有效药物。初步的证据也表明,哌替啶与α2肾上腺素能受体。作者因此研究哌替啶的绑定并激活每个α(2)肾上腺素受体亚型在转染细胞系统。方法:哌替啶的结合能力和抑制forskolin-stimulated环腺苷酸的形成是由三个α(2)肾上腺素受体亚型是暂时性的转染到COS-7细胞已经被测试。阿片拮抗剂纳洛酮和α的能力(2)肾上腺素能受体拮抗剂育亨宾和RX821002阻止哌替啶镇痛作用的抗也评估。哌替啶的能力适应α肾上腺素受体(2 b)评估使用分子建模技术。结果:哌替啶绑定到所有alpha2-adrenoceptor亚型,α(2 b)具有最高的亲和力(α(2 b), 8.6 + / - 0.3 microm;α(2 c), microm 13.6 + / - 1.5, P < 0.05;α(2 a), 38.6 + / - 0.7 microm)。 Morphine was ineffective at binding to any of the receptor subtypes. Meperidine inhibited the production of forskolin-stimulated cyclic adenosine monophosphate mediated by all receptor subtypes but was most effective at the alpha(2B) adrenoceptor (alpha(2B), 0.6 microm; alpha(2A), 1.3 mm; alpha(2C), 0.3 mm), reaching the same level of inhibition (approximately 70%) as achieved with the alpha2-adrenoceptor agonist dexmedetomidine. The analgesic action of meperidine was blocked by naloxone but not by the alpha 2-adrenoceptor antagonists yohimbine and RX821002. The modeling studies demonstrated that meperidine can fit into the alpha(2B)-adrenoceptor subtype. CONCLUSION: Meperidine is a potent agonist at the alpha2 adrenoceptors at its clinically relevant concentrations, especially at the alpha(2B)-adrenoceptor subtype. Activation of the alpha(2B) receptor does not contribute significantly to the analgesic action of meperidine. This raises the possibility that some of its actions, such as antishivering, are transduced by this mechanism.

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药物靶点

药物	目标	类	生物	药理作用	行动
育亨宾	Alpha-2B肾上腺素能受体	蛋白质	人类	是的	拮抗剂	细节