机构:
Univ Sydney, Fac Pharm, Sydney, NSW 2006, AustraliaUniv Sydney, Fac Pharm, Sydney, NSW 2006, Australia
Chebib, M
[1
]
机构:
[1] Univ Sydney, Fac Pharm, Sydney, NSW 2006, Australia
来源:
CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY
|
2004年
/
31卷
/
11期
关键词:
GABA(C) receptors;
ligand-gated ion channels;
site-directed mutagenesis;
structure-activity relationship studies;
D O I:
10.1111/j.1440-1681.2004.04083.x
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
1. The present review gives an overview of studies conducted on GABA(C) receptors over the past 10 years since the author started at the University of Sydney. It concentrates on the structure-activity relationship profiles of the receptor and how these studies were used to: (i) develop selective GABA(C) receptor ligands; and (ii) understand the impact of amino acid changes on GABA(C) receptor pharmacology and function. 2. Structure-activity relationship studies involving variations of both ligands and their receptor targets are vital to the discovery of drugs that interact selectively with particular native and mutant receptor subtypes. Such agents may be useful for treating anxiety, depression, epilepsy and memory related disorders, such as Alzheimer's disease.