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51014-29-0

中文名稱 異去氫鉤藤堿
英文名稱 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 2024/10/25 15:17:16
51014-29-0 結(jié)構(gòu)式 51014-29-0 結(jié)構(gòu)式

基本信息

中文別名
異去氫鉤藤堿
異柯諾辛因堿
異去氫鉤藤堿(標(biāo)準(zhǔn)品)
異去氫鉤藤堿?, BR
異去氫鉤藤堿(異柯諾辛因堿 )
ISOCORYNOXEINE 異去氫鉤藤堿
英文別名
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
所屬類別
生物化工:中草藥成分

物理化學(xué)性質(zhì)

外觀性狀白色結(jié)晶粉末,可溶于甲醇、乙醇、DMSO等有機(jī)溶劑,來源于鉤藤。
沸點(diǎn)562.7±50.0 °C(Predicted)
密度1.25
溶解度DMSO : 50 mg/mL (130.74 mM; Need ultrasonic)
酸度系數(shù)(pKa)13.54±0.60(Predicted)
形態(tài)粉末
顏色White to off-white

應(yīng)用領(lǐng)域

用途1
異去氫鉤藤堿具有鎮(zhèn)痛 鎮(zhèn)靜催眠的作用。

常見問題列表

藥理活性
異去氫鉤藤堿為鉤藤堿的一種,異去氫鉤藤堿( isocorynoxeine) 是中藥鉤藤中主要生物堿類成分之一,具有降壓、鎮(zhèn)靜、抗驚厥和神經(jīng)元保護(hù)等藥理活性,是鉤藤中治療高血壓的有效成分。目前對異去氫鉤藤堿在體內(nèi)代謝研究較少。
生物活性
Isocorynoxeine (7-Isocorynoxeine)是一種在鉤藤(Uncaria rhynchophylla)中發(fā)現(xiàn)的主要生物堿,對心、腦血管系統(tǒng)具有廣泛的有益作用。Isocorynoxeine 可抑制 5-HT2A receptor 介導(dǎo)的電流反應(yīng),IC50值為72.4 μM。
靶點(diǎn)

5-HT 2A Receptor

72.4 μM (IC 50 )

體外研究

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.

體內(nèi)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].

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