"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

• 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.