Transporters as Targets for Drugs (eBook)

Susan Napier, Matilda Bingham (Herausgeber)

eBook Download: PDF

2009 | 2009
XIV, 254 Seiten
Springer Berlin (Verlag)
978-3-540-87912-1 (ISBN)

Infos

In each volume of Transporters as Targets for Drugs an overview chapter introduces the newcomer to the topic covered. The series covers hot topics of frontier research summarized by reputed scientists in the field.

Inhalt

Volume Editors 5
Editorial Board 5
Topics in Medicinal Chemistry Also Available Electronically 6
Preface to the Series 7
Preface to Volume 4 8
Contents 9
Overview: Transporters as Targets for Drug Discovery 10
1 Introduction 11
2 Transporter Classification 11
3 NSS Transporter Assays 14
4 Transporters and Structure-Based Drug Design (SBDD) 15
5 Transporters as Targets for Drug Discovery 17
6 Summary 20
References 20
Membrane Transporters: Structure, Function and Targets for Drug Design 23
1 Introduction 25
2 Membrane Protein Structures 27
3 Membrane Transporter Proteins 28
4 Structure Determination of Membrane Proteins 32
5 Transporters of Known 3D Structure 37
6 Potential for New Drug Development 44
7 Conclusions 54
References 55
Design of Monoamine Reuptake Inhibitors: SSRIs, SNRIs and NRIs 60
1 Introduction 61
2 Selective Serotonin Reuptake Inhibitors 64
3 Dual Serotonin and Noradrenaline Reuptake Inhibitors 72
4 Noradrenaline Reuptake Inhibitors 87
5 Conclusions 98
References 98
Atypical Dopamine Uptake Inhibitors that Provide Clues About Cocaine’s Mechanism at the Dopamine Transporter 102
1 Introduction –Chemical and Pharmacological Diversity of Dopamine Uptake Inhibitors 103
2 Case Study: Benztropine Analogues 104
3 Design, Synthesis and SAR of the Benztropine Analogues 106
4 In Vivo Findings 116
5 Mechanisms for Differences with Cocaine 121
6 Preclinical Assessment of Cocaine-Abuse Therapy 130
7 Summary and Conclusions 133
References 134
The Design, Synthesis and Structure–Activity Relationship of Mixed Serotonin, Norepinephrine and Dopamine Uptake Inhibitors 137
1 Introduction 138
2 Overview of Dual-Uptake Inhibitors 140
3 Design, Synthesis and Structure– Activity Relationship of Triple- Uptake Inhibitors 143
4 Conclusions 157
References 158
Molecular Imaging of Transporters with Positron Emission Tomography 161
1 Introduction 163
2 PET Principles 164
3 PET Studies of Transporters 170
4 Conclusions 186
References 187
Pharmacology of Glutamate Transport in the CNS:Substrates and Inhibitorsof Excitatory Amino Acid Transporters (EAATs)and the Glutamate/Cystine Exchanger System x–c 193
1 Introduction 195
2 Excitatory Amino Acid Transporters (EAATs) 196
3 System x–c : Cystine/Glutamate Exchanger 214
References 223
Glycine Transporters and Their Inhibitors 229
1 Introduction 230
2 Glycine Transporter Isoforms 230
3 Distribution 231
4 Function 232
5 Therapeutic Potential 233
6 Medicinal Chemistry of Glycine Transporter Inhibitors 235
7 Conclusion 247
References 247
Subject Index 254

Produkt-Details

• Erscheint lt. Verlag: 5.5.2009
• Reihe/Serie: Topics in Medicinal Chemistry
• Reihe/Serie: Topics in Medicinal Chemistry
• Zusatzinfo: XIV, 254 p. 109 illus., 11 illus. in color.
• Verlagsort: Berlin
• Sprache: englisch
• Themenwelt: Studium ► 1. Studienabschnitt (Vorklinik) ► Biochemie / Molekularbiologie
• Themenwelt: Naturwissenschaften ► Biologie
• Themenwelt: Naturwissenschaften ► Chemie
• Themenwelt: Technik
• Schlagworte: Cocaine • dopamine • medicinal chemistry • Molecular Chemistry • Organic Chemistry • Pharmaceutical Chemistry • Pharmacy
• ISBN-10: 3-540-87912-9 / 3540879129
• ISBN-13: 978-3-540-87912-1 / 9783540879121