Molecular Neuropharmacology: Strategies and Methods / Edition 1

by Arne Schousboe, Hans Bräuner-Osborne

Overview

A powerful collection of readily reproducible cutting-edge techniques for characterizing the ligand or substrate binding of neurotransmitter receptors and transporters. The procedures cover interdisciplinary interactions for monoamine transporters, amino acid transporters, ionotropic receptors, metabotropic glutamate receptors, GABA receptors, and other G protein-coupled receptors. By illuminating how neurons in the central nervous communicate with other, these techniques can lead to the development of novel therapeutic strategies for neurological diseases.

Product Details

ISBN-13:	9781588291431
Publisher:	Springer-Verlag New York, LLC
Publication date:	12/22/2003
Edition description:	2004
Pages:	271
Product dimensions:	7.01(w) x 10.00(h) x 0.04(d)

Table of Contents

I. Molecular Pharmacology of Glutamate Receptors.- 1 Computational Studies of Ligand-Receptor Interactions in Ionotropic Glutamate Receptors.- 2 Delineation of the Physiological Role of Kainate Receptors by Use of Subtype Selective Ligands.- 3 Molecular Pharmacology of the Metabotropic Glutamate Receptors.- II. Molecular Pharmacology of GABA Receptors.- 4 Functional Characterization of GABAA Receptor Ligands In Vitro: Correlation With In Vivo Activity.- 5 In Vivo Function of GABAA Receptor Subtypes Unraveled With Mutant Mice.- 6 Characterization of the GABAA Receptor Recognition Site Through Ligand Design and Pharmacophore Modeling.- 7 The GABAB Receptor: From Cloning to Knockout Mice.- III. Molecular Pharmacology of Transmitter Transporters.- 8 Structure and Molecular Characterization of the Substrate-Binding Sites of the Dual-Function Glutamate Transporters.- 9 Allosteric Modulation of Glutamate Transporters.- 10 Characterization of the Substrate-Binding Site in GABA Transporters.- 11 Insights From Endogenous and Engineered Zn2+ Binding Sites in Monoamine Transporters.- 12 A Structural Context for Studying Neurotransmitter Transporter Function.- 13 Functional Mechanisms of G Protein-Coupled Receptors in a Structural Context.

Editorial Reviews

Reviewer: Thomas L. Pazdernik, PhD (University of Kansas Medical Center)
Description: A pharmacologist and medicinal chemist, both with excellent reputations, recruited a team of experts to write chapters on the molecular pharmacology of glutamate and GABA receptors as well as transmitter transporters. Their goal is to correlate information obtained from the cloning of receptors and transporters with expertise from medicinal and computational chemistry to enhance the understanding of the interaction of ligands with macromolecules.
Purpose: The purpose is to use the knowledge gained by molecular pharmacologists and medicinal chemists to enhance the understanding of the interaction of ligands with macromolecules. This collection of chapters successfully bridges the gap between molecular biology and advanced chemistry and is very well done and much needed.
Audience: This book will be extremely valuable to both academic and industrial scientists who are interested in the molecular and chemical aspects of receptor and transmitter function as well as the those involved in the design of drugs that will selectively interact with the receptors and transporters discussed. This book will also be very valuable for graduate students in either the biomedical or chemical sciences who are studying transporters or receptors.
Features: The book is divided into three parts with chapters on the molecular pharmacology of glutamate receptors, molecular pharmacology of GABA receptors, and molecular pharmacology of transmitter transporters. Each chapter is well written and concise beginning with an appropriate introduction to the topic and ending with a brief summary, conclusion, or future perspective section. The references are selective and appropriate. Special features include cutting-edge techniques for using site directed mutagenesis and molecular modeling; novel insights into the functioning of transmitter receptors and transporters; and state-of-the-art discussions on the molecular pharmacology of GABA and glutamate receptors and transmitter transporters. Eleven color figures illustrate the molecular structure of receptors and transporters, including a figure with reference to the Arcadia Institute for Computation Biomedicine Website. Information on X-ray crystallography is included when available.
Assessment: I would highly recommend this book to neuroscientists, pharmacologists, and medicinal chemists who are interested in ligand-macromolecular interactions. It provides descriptions of state-of-the-art tools needed to understand how CNS neurons communicate and perspectives regarding the development of novel therapeutic drugs for neurological diseases.

Doody's Review Service

4 Stars! from Doody

"I would highly recommend this book to neuroscientists, pharmacologists, and medicinal chemists who are interested in ligand-macromolecular interactions. It provides descriptions of state-of-the-art tools needed to understand how CNS neurons communicate and perspectives regarding the development of novel therapeutic drugs for neurological diseases. Each chapter is well written and concise beginning with an appropriate introduction to the topic and ending with a brief summary, conclusion, or future perspective section. The references are selective and appropriate. Special features include cutting-edge techniques for using site directed mutagenesis and molecular modeling; novel insights into the functioning of transmitter receptors and transporters; and state-of-the-art discussions on the molecular pharmacology of GABA and glutamate receptors and transmitter transporters. "-Doody's Health Sciences Book Review Journal

"...provides a highly readable account...an excellent book." - ChemBioChem

From the Publisher