GABA(A)-receptor subtypes: Clinical efficacy and selectivity of benzodiazepine site ligands

被引：81

作者：

Korpi, ER

Mattila, MJ

Wisden, W

Luddens, H

机构：

[1] UNIV HELSINKI,INST BIOMED,DEPT PHARMACOL & TOXICOL,HELSINKI,FINLAND

[2] MRC CTR,MOL BIOL LAB,CAMBRIDGE,ENGLAND

[3] UNIV MAINZ,DEPT PSYCHIAT,CLIN RES GRP,D-6500 MAINZ,GERMANY

来源：

ANNALS OF MEDICINE | 1997年 / 29卷 / 04期

关键词：

anxiety; benzodiazepines; GABA(A) receptor; partial agonism; sleep induction; subtype selectivity;

D O I：

10.3109/07853899708999348

中图分类号：

R5 [内科学];

学科分类号：

1002 [临床医学]; 100201 [内科学];

摘要：

The main inhibitory neurotransmitter receptor of the brain, the gamma-aminobutyric acid type A receptor (GABA(A)), mediates the actions of several classes of clinically important drugs, such as benzodiazepines, barbiturates and general anaesthetics. This review summarizes the current knowledge on how classical benzodiazepines and novel nonbenzodiazepine compounds act on the benzodiazepine site of GABA, receptors and on their clinical pharmacology related to anxiolytic, sedative, hypnotic and cognitive effects or side-effects. Partial agonism, receptor subtype selectivity and novel binding sites are discussed as possible strategies to develop new drugs with fewer adverse effects than are seen in the clinical use of benzodiazepines.

引用

页码：275 / 282

页数：8

共 65 条

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Comparative study of the effects of zopiclone (7.5 mg), zolpidem, flunitrazepam and a placebo on nocturnal cognitive performance in healthy subjects, in relation to pharmacokinetics [J].