Voltage-Gated Ion Channels as Drug Targets

✍ Scribed by Theodor Dingermann, Dieter Steinhilber, Gerd Folkers, Raimund Mannhold, Hugo Kubinyi

• Publisher: Wiley-VCH
• Year: 2004
• Tongue: English
• Leaves: 488
• Series: Methods and Principles in Medicinal Chemistry 29
• Edition: 1
• Category: Library

✦ Synopsis

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

✦ 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