LEADER 05289nam 2200625Ia 450 001 9910830490903321 005 20170810191502.0 010 $a1-280-72345-9 010 $a9786610723454 010 $a3-527-60814-1 010 $a3-527-60774-9 035 $a(CKB)1000000000376652 035 $a(EBL)481467 035 $a(SSID)ssj0000312869 035 $a(PQKBManifestationID)11224061 035 $a(PQKBTitleCode)TC0000312869 035 $a(PQKBWorkID)10332534 035 $a(PQKB)11505439 035 $a(MiAaPQ)EBC481467 035 $a(OCoLC)85821182 035 $a(EXLCZ)991000000000376652 100 $a20060220d2006 uy 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 00$aVoltage-gated ion channels as drug targets$b[electronic resource] /$fedited by David J. Triggle ...[et al.] 210 $aWeinheim $cWiley VCH ;$a[Chichester $cJohn Wiley]$dc2006 215 $a1 online resource (493 p.) 225 1 $aMethods and principles in medicinal chemistry ;$v29 300 $aDescription based upon print version of record. 311 $a3-527-31258-7 320 $aIncludes bibliographical references and index. 327 $aVoltage-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 327 $a3.4 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 327 $a4.3 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 327 $a5.1.3 Distribution of VGCCs and their Physiological Roles5.1.4 Structure of VGCC ?(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-?-subunit Sites; 5.3.6 Calcium Antagonism through Gene Delivery 327 $a5.4 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 327 $a6.2.1 Drugs that Act on Sodium Channels 330 $aEdited by the most prominent person in the field and top researchers at US pharmaceutical companies, this is a unique resource for drug developers and physiologists seeking a molecular-level understanding of ion channel pharmacology. After an introduction to the topic, the authors evaluate the structure and function of ion channels, as well as related drug interaction. A section on assay technologies is followed by a section each on calcium, sodium and potassium channels. Further chapters cover genetic and acquired channelopathies, before the book closes with a look at safety issues in ion 410 0$aMethods and principles in medicinal chemistry ;$v29. 606 $aIon channels 606 $aMembranes (Biology) 615 0$aIon channels. 615 0$aMembranes (Biology) 676 $a571.64 701 $aTriggle$b D. J$01622634 801 0$bMiAaPQ 801 1$bMiAaPQ 801 2$bMiAaPQ 906 $aBOOK 912 $a9910830490903321 996 $aVoltage-gated ion channels as drug targets$93956605 997 $aUNINA