异去氢钩藤碱

药理活性生物活性靶点体外研究体内研究异去氢钩藤碱试剂级价格

异去氢钩藤碱

CAS号:51014-29-0
英文名:Isocorynoxeine
中文名:异去氢钩藤碱
CBNumber:CB41483206
分子式:C22H26N2O4
分子量:382.46
MOL File:51014-29-0.mol

异去氢钩藤碱化学性质

沸点 :562.7±50.0 °C(Predicted)
密度 :1.25
溶解度 :DMSO : 50 mg/mL (130.74 mM; Need ultrasonic)
形态 :Powder
酸度系数(pKa) :13.54±0.60(Predicted)
颜色 :White to off-white

异去氢钩藤碱性质、用途与生产工艺

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。