Voltage-gated ion channels as drug targets [[electronic resource] /] / edited by David J. Triggle ...[et al.]

• Pubblicazione: Weinheim, : Wiley VCH; [Chichester, : John Wiley], c2006
• Descrizione fisica: 1 online resource (493 p.)
• Disciplina: 571.64
• Soggetto topico: Ion channels; Membranes (Biology)
• Altri autori: TriggleD. J
• Note generali: Description based upon print version of record.
• Nota di bibliografia: Includes bibliographical references and index.
• Nota di contenuto: Voltage-Gated Ion Channels as Drug Targets; Contents; Preface; 1 Introduction - On Ion Channels; 2 The Voltage-gated Ion Channel Superfamily; 2.1 Introduction; 2.2 Voltage-gated Sodium Channels; 2.3 Voltage-gated Calcium Channels; 2.4 Voltage-gated Potassium Channels; 2.5 Inwardly Rectifying Potassium Channels; 2.6 Common Aspects of Ion Channel Structure and Function; 2.7 Conclusions; 3 State-dependent Drug Interactions with Ion Channels; 3.1 Introduction; 3.2 Ion Channels as Drug Receptors; 3.3 Ion Channels Adopt Multiple Conformations ; 3.4 Biophysics Meets Pharmacology: State Dependence, Voltage Dependence, and the Modulated Receptor Model3.5 Use Dependence; 3.6 Physical Meaning of State Dependence; 3.7 State Dependence in Drug Discovery; 3.8 Future Directions for Ion Channel Drug Discovery; 4 Assay Technologies: Techniques Available for Quantifying Drug-Channel Interactions; 4.1 Introduction; 4.2 Patch Clamp; 4.2.1 Basic Description of Technique; 4.2.2 Advantages and Disadvantages of Manual Patch Clamp; 4.2.3 Use of Patch Clamp for Quantification of Drug-Channel Effects; 4.2.4 Caveats of Interpretations in Patch Clamp ; 4.3 Planar Patch Clamp4.4 Two-electrode Voltage Clamp (TEVC) of Xenopus Oocytes; 4.5 Membrane Potential Sensing Dyes; 4.5.1 Basic Description of Membrane Potential-sensing Dyes; 4.5.2 Advantages and Disadvantages of Membrane Potential-sensing Dyes; 4.6 Binding; 4.7 Ion Flux; 4.7.1 Fluorescent Indicators of Ion Flux; 4.7.2 Direct Measurement of Ion Flux; 4.8 What Technologies Cannot be Used ... Yet?; 4.9 Summary; 5 Calcium Channels; 5.1 Overview of Voltage-gated Calcium Channels; 5.1.1 Introduction; 5.1.2 Native and Cloned Calcium Channels: Nomenclature and Classification ; 5.1.3 Distribution of VGCCs and their Physiological Roles5.1.4 Structure of VGCC α(1) Subunits; 5.1.5 VGCC Modulation; 5.1.6 VGCCs: Channelopathies and Pathologies; 5.1.7 Summary; 5.2 Drugs Active at T-type Ca(2+) Channels; 5.2.1 Introduction; 5.2.2 Methodology; 5.2.3 Indications; 5.2.4 Conclusions; 5.3 L-type Calcium Channels; 5.3.1 Introduction; 5.3.2 Drugs that Interact with L-type Channels; 5.3.3 Specific Drug Classes; 5.3.4 Other Drug Classes Active at Ca(V)1 Channels; 5.3.5 Drug Interactions at Non-α-subunit Sites; 5.3.6 Calcium Antagonism through Gene Delivery ; 5.4 N-type Calcium Channels5.4.1 Introduction; 5.4.2 N-type Calcium Channel Pharmacology; 5.4.3 Inorganic Cations; 5.4.4 Peptide Blockers; 5.4.5 Small Organic Molecule N-type Blockers; 5.4.6 Conclusions; 6 Sodium Channels; 6.1 Molecular, Biophysical and Functional Properties of Voltage-gated Sodium Channels; 6.1.1 Introduction; 6.1.2 Primary and Tertiary Structure; 6.1.3 Sodium Channel Expression; 6.1.4 Biophysical Properties of Voltage-dependent Sodium Channels; 6.1.5 Disease Association; 6.1.6 Conclusions; 6.2 Small Molecule Blockers of Voltage-gated Sodium Channels ; 6.2.1 Drugs that Act on Sodium Channels
• Sommario/riassunto: Edited by the most prominent person in the field and top researchers at US pharmaceutical companies, this is a unique resource for drug developers and physiologists seeking a molecular-level understanding of ion channel pharmacology. After an introduction to the topic, the authors evaluate the structure and function of ion channels, as well as related drug interaction. A section on assay technologies is followed by a section each on calcium, sodium and potassium channels. Further chapters cover genetic and acquired channelopathies, before the book closes with a look at safety issues in ion
• Titolo autorizzato: Voltage-gated ion channels as drug targets
• ISBN: 1-280-72345-9; 9786610723454; 3-527-60814-1; 3-527-60774-9
• Formato: Materiale a stampa
• Livello bibliografico: Monografia
• Lingua di pubblicazione: Inglese
• Record Nr.: 9910830490903321
• Lo trovi qui: Univ. Federico II
• Serie: Methods and principles in medicinal chemistry ; ; 29.