Semisynthetic preparation of amentoflavone:: A negative modulator at GABAA receptors

被引：42

作者：

Hanrahan, JR ^{[1
]}

Chebib, M

Davucheron, NLM

Hall, BJ

Johnston, GAR

机构：

[1] Univ Sydney, Fac Pharm, Sydney, NSW 2006, Australia

[2] Univ Sydney, Dept Pharmacol, Sydney, NSW 2006, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(03)00434-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amentoflavone is found in a number of plants with medicinal properties, including Ginkgo biloba and Hypericum perforatum (St. John's Wort). We have developed a rapid and economic semi-synthetic preparation of amentoflavone from biflavones isolated from autumnal Ginkgo biloba leaves. Several studies have shown that amentoflavone binds to benzodiazepine receptors. Using two electrode voltage-clamp methodology, amentoflavone has been shown to be a negative modulator of GABA at GABA(A) alpha(1)beta(2)gamma(2L) receptors expressed in Xenopus laevis oocytes This action appears to be independent of the flumazenil-sensitive benzodiazepine modulatory sites on the GABAA receptor. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2281 / 2284

页数：4

共 14 条

[1]

BAUREITHEL KH, 1997, PHARM ACTA HELV, V7, P153

[2] In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs [J].