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Ion Channel book from C.H.I.P.S.

Voltage-Gated Ion Channels as Drug Targets
by David J. Triggle

Voltage-Gated Ion Channels as Drug Targets evaluates the structure and function of ion channels, as well as related drug interaction.

Contents

Introduction

The Voltage-gated Ion Channel Superfamily

  • Voltage-gated Sodium Channels
  • Voltage-gated Calcium Channels
  • Voltage-gated Potassium Channels
  • Inwardly Rectifying Potassium Channels
  • Common Aspects of Ion Channel Structure and Function

State-dependent Drug Interactions with Ion Channels

  • Ion Channels as Drug Receptors
  • Ion Channels as Adopt Multiple Conformations
  • Biophysics Meets Pharmacology: State Dependence, Voltage Dependence, and the Modulated Receptor Model
  • Use Dependence
  • Physical Meaning of State Dependence
  • State Dependence in Drug Discovery
  • Future Directions for Ion Channel Drug Discovery

Assay Technologies: Techniques Available for Quantifying Drug-Channel Interactions

  • Patch Clamp
  • Planar Patch Clamp
  • Two-electrode Voltage Clamp (TEVC) of Xenopus Oocytes
  • Membrane Potential Sensing Dyes
  • Binding
  • Ion Flux
  • What Technologies Cannot be Used... Yet?

Calcium Channels

  • Overview of Voltage-gated Calcium Channels
  • Drugs Active at T-type Ca2+ Channels
  • L-type Calcium Channels
  • N-type Calcium Channels

Sodium Channels

  • Molecular, Biophysical and Functional Properties
  • Small Molecule Blockers of Voltage-gated Sodium Channels

Potassium Channels

  • Potassium Channels: Overview of Molecular, Biophysical and Pharmacological Properties
  • Kv1.3 Potassium Channel: Physiology, Pharmacology and Therapeutic Indications
  • Drugs Active at Kv1.5 Potassium Channels
  • Medicinal Chemistry of Ca2+-activated K+ Channel Modulators
  • Drugs Active at ATP-sensitive K+ Channels
  • Compounds that Activate KCNQ(2-5) Family of Potassium Ion Channels

Genetic and Acquired Channelopathies

  • Inherited Disorders of Ion Channels
  • Structural and Ligand-based Models for HERG and their Application in Medicinal Chemistry
  • Ion Channel Safety Issues in Drug Development

Index

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Voltage-Gated Ion Channels as Drug Targets
by David J. Triggle
2006 479 pages $214.00 + shipping
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