51014-29-0

中文名称异去氢钩藤碱

英文名称 Isocorynoxeine

CAS 51014-29-0

分子式 C22H26N2O4

分子量 382.46

MOL 文件 51014-29-0.mol

更新日期 2024/06/07 15:03:47

51014-29-0 结构式

基本信息物理化学性质应用领域常见问题列表

基本信息

中文别名

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

英文别名

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

物理化学性质

外观性状白色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于钩藤。

沸点562.7±50.0 °C(Predicted)

密度1.25

溶解度DMSO : 50 mg/mL (130.74 mM; Need ultrasonic)

酸度系数(pKa)13.54±0.60(Predicted)

形态粉末

应用领域

用途1

异去氢钩藤碱具有镇痛镇静催眠的作用。

常见问题列表

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].