1;Volume Editors;5 2;Editorial Board;5 3;Topics in Medicinal Chemistry Also Available Electronically;6 4;Preface to the Series;7 5;Preface to Volume 4;8 6;Contents;9 7;Overview: Transporters as Targets for Drug Discovery;10 7.1;1 Introduction;11 7.2;2 Transporter Classification;11 7.3;3 NSS Transporter Assays;14 7.4;4 Transporters and Structure-Based Drug Design (SBDD);15 7.5;5 Transporters as Targets for Drug Discovery;17 7.6;6 Summary;20 7.7;References;20 8;Membrane Transporters: Structure, Function and Targets for Drug Design;23 8.1;1 Introduction;25 8.2;2 Membrane Protein Structures;27 8.3;3 Membrane Transporter Proteins;28 8.4;4 Structure Determination of Membrane Proteins;32 8.5;5 Transporters of Known 3D Structure;37 8.6;6 Potential for New Drug Development;44 8.7;7 Conclusions;54 8.8;References;55 9;Design of Monoamine Reuptake Inhibitors: SSRIs, SNRIs and NRIs;60 9.1;1 Introduction;61 9.2;2 Selective Serotonin Reuptake Inhibitors;64 9.3;3 Dual Serotonin and Noradrenaline Reuptake Inhibitors;72 9.4;4 Noradrenaline Reuptake Inhibitors;87 9.5;5 Conclusions;98 9.6;References;98 10;Atypical Dopamine Uptake Inhibitors that Provide Clues About Cocaine's Mechanism at the Dopamine Transporter;102 10.1;1 Introduction -Chemical and Pharmacological Diversity of Dopamine Uptake Inhibitors;103 10.2;2 Case Study: Benztropine Analogues;104 10.3;3 Design, Synthesis and SAR of the Benztropine Analogues;106 10.4;4 In Vivo Findings;116 10.5;5 Mechanisms for Differences with Cocaine;121 10.6;6 Preclinical Assessment of Cocaine-Abuse Therapy;130 10.7;7 Summary and Conclusions;133 10.8;References;134 11;The Design, Synthesis and Structure-Activity Relationship of Mixed Serotonin, Norepinephrine and Dopamine Uptake Inhibitors;137 11.1;1 Introduction;138 11.2;2 Overview of Dual-Uptake Inhibitors;140 11.3;3 Design, Synthesis and Structure- Activity Relationship of Triple- Uptake Inhibitors;143 11.4;4 Conclusions;157 11.5;References;158 12;Molecular Imaging of Transporters with Positron Emission Tomography;161 12.1;1 Introduction;163 12.2;2 PET Principles;164 12.3;3 PET Studies of Transporters;170 12.4;4 Conclusions;186 12.5;References;187 13;Pharmacology of Glutamate Transport in the CNS:Substrates and Inhibitorsof Excitatory Amino Acid Transporters (EAATs)and the Glutamate/Cystine Exchanger System x-c;193 13.1;1 Introduction;195 13.2;2 Excitatory Amino Acid Transporters (EAATs);196 13.3;3 System x-c : Cystine/Glutamate Exchanger;214 13.4;References;223 14;Glycine Transporters and Their Inhibitors;229 14.1;1 Introduction;230 14.2;2 Glycine Transporter Isoforms;230 14.3;3 Distribution;231 14.4;4 Function;232 14.5;5 Therapeutic Potential;233 14.6;6 Medicinal Chemistry of Glycine Transporter Inhibitors;235 14.7;7 Conclusion;247 14.8;References;247 15;Subject Index;254