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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