Modifying quinolone antibiotics yields new anxiolytics

被引：38

作者：

Johnstone, TBC

Hogenkamp, DJ

Coyne, L

Su, JP

Halliwell, RF

Tran, MB

Yoshimura, RF

Li, WY

Wang, J

Gee, KW ^{[1
]}

机构：

[1] Univ Calif Irvine, Coll Med, Dept Pharmacol, Irvine, CA 92697 USA

[2] Univ Durham, Sch Biol & Biomed Sci, Durham DH1 3LE, England

[3] Univ Pacific, Thomas J Long Sch Pharm & Hlth Sci, Stockton, CA 95211 USA

来源：

NATURE MEDICINE | 2004年 / 10卷 / 01期

关键词：

D O I：

10.1038/nm967

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Patients taking fluoroquinolone antibiotics such as norfloxacin exhibit a low incidence of convulsions and anxiety. These side effects probably result from antagonism of the neurotransmitter gamma-aminobutyric acid (GABA) at the brain GABA(A) receptor complex (GRC). Modification of norfloxacin yields molecules such as compound 4 that potentiate GABA action with alpha(2) subunit selectivity. Compound 4 is anxiolytic but does not cause sedation, and may represent a new class of ligands that have anxiolytic activity without sedative liability.

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收藏

页码：31 / 32

页数：2

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