The GABA Receptors

This volume is the third edition of a monograph series that was first published in 1983. The demand for this work is a testament to the impact of studies on -aminobutyric acid (GABA) receptors on the basic understanding of synaptic transmission and on defining the clinical importance of the neurotransmitter system. Chronicled in The GABA Receptors, Third Edition, are the advances made in understanding the molecular and pharmacological properties of GABA A and GABA receptors since the topic was last reviewed in 1996. Particular B emphasis is placed on describing the assembly, structure, and function of GABA B sites, the first heterodimeric G protein-coupled receptors identified in vivo. In addition, there are reports dealing with the subunit composition, trafficking, and pharmacological selectivity of GABA receptors. Aside from providing A insights into the fundamental properties of ligand-gated ion channels and second messenger systems, the findings detailed in this work point the way for developing novel therapeutics capable of more selectively manipulating these transmitter sites.

This volume presents a critical appraisal of the current understanding of the molecular, behavioral, biochemical, clinical, and pharmacological properties of GABA receptors. It places emphasis on exploring cutting-edge findings on the structural properties of receptor sites, mechanisms of receptor expression, chemical agents that differentiate receptor subtypes, and phenotypes displayed by GABA receptor null mice. Chapters in this updated and expanded edition examine such topics as GABA receptor subtypes, trafficking postsynaptic GABA receptors, GABA receptor mutations associated with idiopathic generalized epilepsies and febrile seizures, and GABA receptors as a potential therapeutic target.

The GABA Receptors.- Functional Relevance of GABAA-Receptor Subtypes.- Trafficking of Postsynaptic GABAA Receptors by Receptor-Associated Proteins.- Subunit Composition and Structure of GABAA-Receptor Subtypes.- Differential Activation of GABAA-Receptor Subtypes.- GABAA-Receptor Mutations Associated With Idiopathic Generalized Epilepsies and Febrile Seizures.- Abuse and Dependence Liability of GABAA-Receptor Modulators.- Mechanisms of GABAA and GABAB Receptor Gene Regulation and Cell Surface Expression.- Chemistry of GABAB Modulators.- The Unusual Functioning of the GABAB-Receptor Heterodimer.- Characteristics of GABAB Receptor Mutant Mice.- GABAB Receptor ad a Potential Therapeutic Target.