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异去氢钩藤碱

更新时间: 2024-09-26 20:45:48 责编:网友投稿 浏览

异去氢钩藤碱

异去氢钩藤碱 用途与合成方法
药理活性异去氢钩藤碱为钩藤碱的一种,异去氢钩藤碱( isocorynoxeine) 是中药钩藤中主要生物碱类成分之一,具有降压、镇静、抗惊厥和神经元保护等药理活性,是钩藤中治疗高血压的有效成分。目前对异去氢钩藤碱在体内代谢研究较少。
生物活性Isocorynoxeine (7-Isocorynoxeine)是一种在钩藤(Uncaria rhynchophylla)中发现的主要生物碱,对心、脑血管系统具有广泛的有益作用。Isocorynoxeine 可抑制 5-HT2A receptor 介导的电流反应,IC50值为72.4 μM。
靶点

5-HT 2A Receptor

72.4 μM (IC 50 )

体外研究

Isocorynoxeine inhibits 5-HT 2A receptor-mediated 5-HT currents. Isocorynoxeine prefer to interact with 5-HT 2A receptors rather than with 5-HT 2C receptors in the brain.Isocorynoxeine exhibits less potent inhibitory activity (with IC 50 values of > 100 μM) against the 5-HT 2C receptor-mediated response than the 5-HT 2A receptor-mediated response in oocytes. Isocorynoxeine dose-dependently and competitively inhibits 5-HT-evoked currents in Xenopus oocytes expressing 5-HT 2A receptors, but has less of a suppressive effect on those in oocytes expressing 5-HT 2C receptors.

体内研究

The effects of Rhynchophylline, Corynoxeine, and Isocorynoxeine, isorhynchophylline-related alkaloids present are tested in Uncaria species, on 5-MeO-DMT-induced head-twitch behaviour in reserpinized mice. Neither Rhynchophylline [H=1.369, P=0.504] nor Corynoxeine [H=0.242, P=0.886] affects the behaviour, while Isocorynoxeine significantly attenuates it at 30 mg/kg (i.p.) [H=7.582, P<0.01].

化学性质 白色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于钩藤。
用途 异去氢钩藤碱具有镇痛 镇静催眠的作用。
用途 用于含量测定/鉴定/药理实验等。
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