异去氢钩藤碱

中文名称:

异去氢钩藤碱

中文同义词:

异去氢钩藤碱(异柯诺辛因碱 );异柯诺辛因碱;异去氢钩藤碱;异去氢钩藤碱(标准品);ISOCORYNOXEINE 异去氢钩藤碱;异去氢钩藤碱?, BR

英文名称:

Isocorynoxeine

英文同义词:

Isocorynoxeine;(16E,20α)-16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester;(alphaE,1S,6R,7S,8aS)-6-ethenyl-1,2,2,3,6,7,8,8a-octahydro-alpha-(methoxymethylene)-2-oxospiro[3H-indole-3,1(5H)-indolizine]-7-acetic acid methyl ester;Isocorynoxeine, BR;Isocorynoxeine (7-Isocorynoxeine);Spiro[3H-indole-3,1(5H)-indolizine]-7-acetic acid, 6-ethenyl-1,2,2,3,6,7,8,8a-octahydro-α-(methoxymethylene)-2-oxo-, methyl ester, (αE,1S,6R,7S,8aS)-;Isocorynoxeine USP/EP/BP

CAS号:

51014-29-0

分子式:

C22H26N2O4

分子量:

382.46

EINECS号:

相关类别:

对照品;植提标准品;中药对照品;标准品;对照品,标准品;植物提取物;中草药成分;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;标准品-中药标准品;生物碱;标准品 -中药标准品;标准品，对照品

Mol文件:

51014-29-0.mol

沸点 

562.7±50.0 °C(Predicted)

密度 

1.25

酸度系数(pKa)

13.54±0.60(Predicted)

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 )

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。