Voltage-Gated Ion Channels as Drug Targets

Theodor Dingermann, Dieter Steinhilber, Gerd Folkers, Raimund Mannhold, Hugo Kubinyi9783527304318, 3-527-30431-2, 3-527-30438-X, 3-527-30678-1, 3-527-30693-5

Content: Introduction : on ion channels / Murali Gopalakrishnan, David Rampe, David Triggle, Wei Zheng — The voltage-gated ion channel superfamily / William A. Catterall — State-dependent drug interactions with ion channels / Stefan I. McDonough, Bruce P. Bean — Assay technologies : techniques available for quantifying drug-channel interactions / Derek Leishman, Gareth Waldron — Overview of voltage-gated calcium channels / Clinton Doering, Gerald Zamponi — Drugs active at T-type Ca²⁺ channels / Thomas M. Connolly, James C. Barrow — L-type calcium channels / David J. Triggle — N-type calcium channels — Molecular, biophysical and functional properties of voltage-gated sodium channels / Douglas S. Krafte, Mark Chapman, Ken McCormack — Small molecule blockers of voltage-gated sodium channels / Jesús E. González, Andreas P. Termin, Dean M. Wilson — Potassium channels : overview of molecular, biophysical and pharmacological properties / Murali Gopalakrishnan, Char-Chang Shieh, Jun Chen — Kv1.3 potassium channel : physiology, pharmacology and therapeutic indications / K. George Chandy, Heike Wulff, Christine Beeton, Peter A. Calabresi, George A. Gutman, Michael Pennington — Drugs active at kv1.5 potassium channels / Stefan Peukert, Heinz Gögelein — Medicinal chemistry of Ca²⁺-activated K⁺ channel modulators / Sean C. Turner, Char-Chang Shieh — Drugs active at ATP-sensitive K⁺ channels / William A. Carroll — Compounds that activate KCNQ(2-5) family of potassium ion channels / Grant McNaughton-Smith, Alan D. Wickenden — Inherited disorders of ion channels / Kate Bracey, Dennis Wray — Structural and ligand-based models for HERG and their application in medicinal chemistry / Yi Li, Giovanni Cianchetta, Roy J. Vaz — Ion channel safety issues in drug development / Armando A. Lagrutta, Joseph J. Salata

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Table of contents :
Cover……Page 1
Voltage-Gated Ion Channels as Drug Targets……Page 2
Methods and Principles in Medicinal Chemistry……Page 3
Copyright……Page 5
Contents……Page 6
Preface……Page 12
1 Introduction – On Ion Channels……Page 14
2 The Voltage-gated Ion Channel Superfamily……Page 19
3 State-dependent Drug Interactions with Ion Channels……Page 31
4 Assay Technologies: Techniques Available for Quantifying Drug–Channel Interactions……Page 49
5.1 Overview of Voltage-gated Calcium Channels……Page 76
5.2 Drugs Active at T-type Ca2+ Channels……Page 95
5.3 L-type Calcium Channels……Page 111
5.4 N-type Calcium Channels……Page 133
6.1 Molecular, Biophysical and Functional Properties of Voltage-gated Sodium Channels……Page 161
6.2 Small Molecule Blockers of Voltage-gated Sodium Channels……Page 178
7.1 Potassium Channels: Overview of Molecular, Biophysical and Pharmacological Properties……Page 203
7.2 Kv1.3 Potassium Channel: Physiology, Pharmacology and Therapeutic Indications……Page 224
7.3 Drugs Active at Kv1.5 Potassium Channels [1]……Page 285
7.4 Medicinal Chemistry of Ca2+-activated K+ Channel Modulators……Page 320
7.5 Drugs Active at ATP-sensitive K+ Channels……Page 345
7.6 Compounds that Activate KCNQ(2–5) Family of Potassium Ion Channels……Page 365
8.1 Inherited Disorders of Ion Channels……Page 391
8.2 Structural and Ligand-based Models for HERG and their Application in Medicinal Chemistry……Page 438
8.3 Ion Channel Safety Issues in Drug Development……Page 454
Index……Page 476