Structure, pharmacology, and function of GABAA receptor subtypes.
摘要：
This chapter describes the structure, pharmacology, and function of γ‐aminobutyric acid type A (GABA A ) receptor subtypes. GABA A receptors are the most important inhibitory transmitter receptors in the central nervous system (CNS). They are chloride channels that can be opened by GABA and modulated by a variety of different drugs, such as benzodiazepines, barbiturates, neuroactive steroids, anesthetics, and convulsants. These receptors are composed of ve subunits that can belong to different subunit classes, giving rise to a large variety of distinct receptor subtypes. Depending on their subunit composition, these receptor subtypes exhibit distinct pharmacological and electrophysiological properties. The chapter reviews new compounds interacting with these receptors and novel receptor subtype‐selective compounds are discussed. The evidence for the function of distinct GABA A receptor subtypes in the brain is also summarized in the chapter. The information on the molecular structure of the extracellular and transmembrane domain of GABA A receptors based on the X‐ray crystallographic structure of the acetylcholine binding protein and on the cryo‐electronmicroscopic structure of the nicotinic acetylcholine receptor is provided in the chapter. This structure contains multiple solvent accessible cavities that are used by a variety of allosteric modulators for their interaction with GABA A receptors, explaining the rich pharmacology of the important receptors.
展开
DOI：
10.1016/S1054-3589(06)54010-4
被引量：
年份：
2006
相似文献
参考文献
引证文献
来源期刊
引用走势
站内活动
辅助模式
引用
文献可以批量引用啦~
欢迎点我试用！
