Holdings: Voltage-gated ion channels as drug targets

Voltage-gated ion channels as drug targets:

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Bibliographic Details
Other Authors:	Triggle, David J. (Editor)
Format:	Book
Language:	English
Published:	Weinheim Wiley-VCH-Verl. 2006
Series:	Methods and principles in medicinal chemistry 29
Subjects:	Canaux ioniques Membranes (Biologie) Drug Delivery Systems Drug Design Ion Channels Ion channels Membranes (Biology) Spannungskontrollierter Ionenkanal Targeted drug delivery Aufsatzsammlung
Online Access:	Inhaltstext Inhaltsverzeichnis
Item Description:	Literaturangaben
Physical Description:	XII, 479 S. Ill., graph. Darst. 25 cm
ISBN:	9783527312580 3527312587

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adam_text	VOLTAGE-GATED ION CHANNELS AS DRUG TARGETS EDITED BY DAVID J. TRIGGLE, MURALI GOPALAKRISHNAN, DAVID RAMPE, AND WEI ZHENG WILEY- VCH WILEY-VCH VERLAG GMBH & CO. KGAA CONTENTS PREFACE XI 1 INTRODUCTION - ON ION CHANNELS 1 MURALI GOPALAKRISHNAN, DAVID RAMPE, DAVID TRIGGLE, AND WEI ZHENG 2 THE VOLTAGE-GATED ION CHANNEL SUPERFAMILY 7 WILLIAM A. CATTERALL 2.1 INTRODUCTION 7 2.2 VOLTAGE-GATED SODIUM CHANNELS 7 2.3 VOLTAGE-GATED CALCIUM CHANNELS 9 2.4 VOLTAGE-GATED POTASSIUM CHANNELS 11 2.5 INWARDLY RECTIFYING POTASSIUM CHANNELS 12 2.6 COMMON ASPECTS OF ION CHANNEL STRUCTURE AND FUNCTION 13 2.7 CONCLUSIONS 14 3 STATE-DEPENDENT DRUG INTERACTIONS WITH ION CHANNELS 19 STEFAN I. MCDONOUGH AND BRUCE P. BEAN 3.1 INTRODUCTION 19 3.2 ION CHANNELS AS DRUG RECEPTORS 20 3.3 ION CHANNELS ADOPT MULTIPLE CONFORMATIONS 21 3.4 BIOPHYSICS MEETS PHARMACOLOGY: STATE DEPENDENCE, VOLTAGE DEPENDENCE, AND THE MODULATED RECEPTOR MODEL 24 3.5 USE DEPENDENCE 28 3.6 PHYSICAL MEANING OF STATE DEPENDENCE 30 3.7 STATE DEPENDENCE IN DRUG DISCOVERY 31 3.8 FUTURE DIRECTIONS FOR ION CHANNEL DRUG DISCOVERY 33 VOLTAGE-GATED ION CHANNELS AS DRUG TARGETS. EDITED BY D. TRIGGLE COPYRIGHT 2006 WILEY-VCH VERLAG GMBH & CO. KGAA, WEINHEIM ISBN 3-527-31258-7 VI CONTENTS 4 ASSAY TECHNOLOGIES: TECHNIQUES AVAILABLE FOR QUANTIFYING DRUG-CHANNEL INTERACTIONS 37 DEREK LEISHMAN AND GARETH WALDRON 4.1 INTRODUCTION 37 4.2 PATCH CLAMP 39 4.2.1 BASIC DESCRIPTION OF TECHNIQUE 39 4.2.2 ADVANTAGES AND DISADVANTAGES OF MANUAL PATCH CLAMP 42 4.2.3 USE OF PATCH CLAMP FOR QUANTIFICATION OF DRUG-CHANNEL EFFECTS 44 4.2.4 CAVEATS OF INTERPRETATIONS IN PATCH CLAMP 47 4.3 PLANAR PATCH CLAMP 48 4.4 TWO-ELECTRODE VOLTAGE CLAMP (TEVC) OF XENOPUS OOCYTES 50 4.5 MEMBRANE POTENTIAL SENSING DYES 51 4.5.1 BASIC DESCRIPTION OF MEMBRANE POTENTIAL-SENSING DYES 52 4.5.2 ADVANTAGES AND DISADVANTAGES OF MEMBRANE POTENTIAL-SENSING DYES 53 4.6 BINDING 56 4.7 ION FLUX 57 4.7.1 FLUORESCENT INDICATORS OF ION FLUX 57 4.7.2 DIRECT MEASUREMENT OF ION FLUX 58 4.8 WHAT TECHNOLOGIES CANNOT BE USED ... YET? 59 4.9 SUMMARY 60 5 CALCIUM CHANNELS 65 5.1 OVERVIEW OF VOLTAGE-GATED CALCIUM CHANNELS 65 CLINTON DOERING AND GERALD ZAMPONI 5.1.1 INTRODUCTION 65 5.1.2 NATIVE AND CLONED CALCIUM CHANNELS: NOMENCLATURE AND CLASSIFICATION 65 5.1.3 DISTRIBUTION OF VGCCS AND THEIR PHYSIOLOGICAL ROLES 66 5.1.4 STRUCTURE OF VGCC A, SUBUNITS 69 5.1.5 VGCC MODULATION 72 5.1.6 VGCCS: CHANNELOPATHIES AND PATHOLOGIES 76 5.1.7 SUMMARY 77 5.2 DRUGS ACTIVE AT T-TYPE CA 2+ CHANNELS 84 THOMAS M. CONNOLLY AND JAMES C. BARROW 5.2.1 INTRODUCTION 84 5.2.2 METHODOLOGY 85 5.2.3 INDICATIONS 92 5.2.4 CONCLUSIONS 94 CONTENTS VII 5.3 L-TYPE CALCIUM CHANNELS 200 DAVID J. TRIGGLE 5.3.1 INTRODUCTION 100 5.3.2 DRUGS THAT INTERACT WITH L-TYPE CHANNELS 100 5.3.3 SPECIFIC DRUG CLASSES 103 5.3.4 OTHER DRUG CLASSES ACTIVE AT CA V L CHANNELS 114 5.3.5 DRUG INTERACTIONS AT NON-A-SUBUNIT SITES 116 5.3.6 CALCIUM ANTAGONISM THROUGH GENE DELIVERY 118 5.4 N-TYPE CALCIUM CHANNELS 122 TERRANCE P. SNUTCH 5.4.1 INTRODUCTION 122 5.4.2 N-TYPE CALCIUM CHANNEL PHARMACOLOGY 123 5.4.3 INORGANIC CATIONS 124 5.4.4 PEPTIDE BLOCKERS 125 5.4.5 SMALL ORGANIC MOLECULE N-TYPE BLOCKERS 132 5.4.6 CONCLUSIONS 140 6 SODIUM CHANNELS 151 6.1 MOLECULAR, BIOPHYSICAL AND FUNCTIONAL PROPERTIES OF VOLTAGE-GATED SODIUM CHANNELS 151 DOUGLAS S. KRAFIE, MARK CHAPMAN, AND KEN MCCORMACK 6.1.1 INTRODUCTION 252 6.1.2 PRIMARY AND TERTIARY STRUCTURE 252 6.1.3 SODIUM CHANNEL EXPRESSION 257 6.1.4 BIOPHYSICAL PROPERTIES OF VOLTAGE-DEPENDENT SODIUM CHANNELS 259 6.1.5 DISEASE ASSOCIATION 262 6.1.6 CONCLUSIONS 265 6.2 SMALL MOLECULE BLOCKERS OF VOLTAGE-GATED SODIUM CHANNELS 168 JESUS E. GONZALEZ, ANDREAS P. TERMIN, AND DEAN M. WILSON 6.2.1 DRUGS THAT ACT ON SODIUM CHANNELS 268 6.2.2 NEW INSIGHTS FOR LAUNCHED COMPOUNDS 270 6.2.3 CHALLENGES OF CURRENT AGENTS 275 6.2.4 COMPOUNDS IN CLINICAL DEVELOPMENT 276 6.2.5 NEW BLOCKERS IN DISCOVERY OR PRE-CLINICAL STAGE 280 6.2.6 EMERGING INDICATIONS AND FUTURE DIRECTIONS 286 VIM CONTENTS 7 POTASSIUM CHANNELS 193 7.1 POTASSIUM CHANNELS: OVERVIEW OF MOLECULAR, BIOPHYSICAL AND PHARMACOLOGICAL PROPERTIES 193 MURALI GOPALAKRISHNAN, CHAR-CHANG SHIEH, AND JUN CHEN 7.1.1 INTRODUCTION 193 7.1.2 CLASSIFICATION AND GENERAL PROPERTIES 194 7.1.3 AUXILIARY SUBUNITS 202 7.1.4 CRYSTAL STRUCTURE 201 7.1.5 K + CHANNELS AND DISEASES 204 7.1.6 LIGANDS INTERACTING WITH K + CHANNELS 204 7.1.7 LIGAND BINDING SITES 206 7.1.8 PEPTIDES AND TOXINS 209 7.1.9 SUMMARY 210 7.2 KVL.3 POTASSIUM CHANNEL: PHYSIOLOGY, PHARMACOLOGY AND THERAPEUTIC INDICATIONS 214 K. GEORGE CHANDY, HEIKE WULFF, CHRISTINE BEETON, PETER A. CALABRESI, GEORGE A. GUTMAN, AND MICHAEL PENNINGTON 7.2.1 INTRODUCTION 214 7.2.2 PEPTIDE INHIBITORS OF KVL.3 216 7.2.3 SMALL MOLECULES INHIBITORS OF KVL.3 222 7.2.4 PHYSIOLOGICAL ROLE OF KVL.3 AND THE EFFECTS OF KVL.3 BLOCKERS 7.2.5 DISEASE INDICATIONS 246 7.2.6 CONCLUSIONS 251 7.3 DRUGS ACTIVE AT KVL.5 POTASSIUM CHANNELS [1] 275 STEFAN PEUKERT AND HEINZ GOGELEIN 7.3.1 STRUCTURE OF THE KVL.5 CHANNEL 275 7.3.2 PHARMACOLOGICAL SIGNIFICANCE OF THE KVL.5 CHANNEL 276 7.3.3 KNOWN DRUGS WITH ACTIVITY ON KVL.5 278 7.3.4 STRUCTURAL CLASSES OF NEW KVL.5 CHANNEL BLOCKERS, THEIR STRUCTURE-ACTIVITY RELATIONSHIP AND PHARMACOLOGY 283 7.3.5 STRATEGIES IN LEAD IDENTIFICATION FOR KVL.5 BLOCKERS 296 7.3.6 SELECTIVITY AGAINST OTHER ION CHANNELS 301 7.3.7 STRUCTURAL BASIS FOR KVL.5 CHANNEL BLOCK 302 7.4 MEDICINAL CHEMISTRY OF CA 2+ -ACTIVATED K + CHANNEL MODULATORS SEAN C. TURNER AND CHAR-CHANG SHIEH 7 A.I INTRODUCTION 310 7.4.2 MEDICINAL CHEMISTRY 318 7.4.3 CONCLUSIONS 329 231 310 7.5 7.5.1 7.5.2 7.5.3 7.5.4 7.5.5 7.5.6 7.5.7 7.6 7.6.1 7.6.2 7.6.3 7.6.4 7.6.5 7.6.6 7.6.7 7.6.8 7.6.9 7.6.10 7.6.11 7.6.12 8 8.1 8.1.1 8.1.2 8.1.3 8.1.4 8.1.5 8.1.6 8.1.7 8.1.8 8.1.9 8.1.10 CONTENTS IX DRUGS ACTIVE AT ATP-SENSITIVE K + CHANNELS 335 WILLIAM A. CARROLL INTRODUCTION 335 MITOCHONDRIAL K ATP CHANNEL OPENERS FOR MYOCARDIAL ISCHEMIA 337 SARC-K ATP BLOCKERS FOR VENTRICULAR ARRHYTHMIA 339 SUR1/KIR6.2 OPENERS FOR DIABETES AND HYPERINSULINEMIA 340 SUR2B/KIR6.2 OPENERS FOR OVERACTIVE BLADDER (OAB) 343 K ATP OPENERS FOR ALOPECIA 348 CONCLUSIONS 348 COMPOUNDS THAT ACTIVATE KCNQ(2-5) FAMILY OF POTASSIUM ION CHANNELS 355 GRANT MCNAUGHTON-SMITH AND ALAN D. WICKENDEN INTRODUCTION 355 FLUPIRTINE, RETIGABINE AND RELATED COMPOUNDS 355 BENZANILIDE, BENZISOXAZOLE AND INDAZOLE DERIVATIVES 360 OXINDOLES AND QUINOLINONES 362 2,4-DISUBSTITUTED PYRIMIDINE-5-CARBOXAMIDES DERIVATIVES 364 CINNAMIDE DERIVATIVES AND ANALOGUES 365 5-CARBOXAMIDE-THIAZOLE DERIVATIVES 370 BENZOTHIAZOLES AS KCNQ(2-5) AGONISTS 372 QUINAZOLINONES DERIVATIVES 373 SALICYLIC ACID DERIVATIVES 375 MELCOFENAMIC ACID AND DICLOFENAC-BASED KCNQ(2-5) AGONISTS 375 SUMMARY 377 GENETIC AND ACQUIRED CHANNELOPATHIES 381 INHERITED DISORDERS OF ION CHANNELS 381 KATE BRACEY AND DENNIS WRAY INTRODUCTION 381 POTASSIUM CHANNELS 383 NON-SELECTIVE CATION CHANNELS 390 TRANSIENT RECEPTOR POTENTIAL (TRP) CHANNELS 392 VOLTAGE-GATED SODIUM CHANNELS 393 NONVOLTAGE-GATED SODIUM CHANNELS 397 CALCIUM CHANNELS 399 CHLORIDE CHANNELS 403 LIGAND-GATED CHANNELS 408 CONCLUSIONS 412 CONTENTS 8.2 STRUCTURAL AND LIGAND-BASED MODELS FOR HERG AND THEIR APPLICATION IN MEDICINAL CHEMISTRY 428 YI LI, GIOVANNI CIANCHETTA, AND ROY J. VAZ 8.2.1 INTRODUCTION: PERSPECTIVE ON THE NECESSITY OF MODELS 428 8.2.2 STRUCTURAL ASPECT OF HERG MODELS 430 8.2.3 LIGAND-BASED CHEMOMETRIC MODELS 430 8.2.4 LIGAND-BASED QSAR MODELS 434 8.2.5 APPLICATION OF MODELS TO IMPROVE SELECTIVITY: CASE STUDIES 434 8.2.6 CONCLUSIONS 440 8.3 ION CHANNEL SAFETY ISSUES IN DRUG DEVELOPMENT 444 ARMANDO A. LAGRUTTA AND JOSEPH J. SALATA 8.3.1 INTRODUCTION 444 8.3.2 REGULATORY-INDUSTRY RELATIONSHIP (ICH); SAFETY PHARMACOLOGY 444 8.3.3 SAFETY ISSUES SPECIFIC TO THE HERG CHANNEL 449 8.3.4 INTEGRATED RISK ASSESSMENT OF DELAYED VENTRICULAR REPOLARIZATION 455 8.3.5 BEYOND QT PROLONGATION 457 8.3.6 ISSUES SPECIFIC TO ION CHANNEL TARGETS 459 INDEX 467
adam_txt	VOLTAGE-GATED ION CHANNELS AS DRUG TARGETS EDITED BY DAVID J. TRIGGLE, MURALI GOPALAKRISHNAN, DAVID RAMPE, AND WEI ZHENG WILEY- VCH WILEY-VCH VERLAG GMBH & CO. KGAA CONTENTS PREFACE XI 1 INTRODUCTION - ON ION CHANNELS 1 MURALI GOPALAKRISHNAN, DAVID RAMPE, DAVID TRIGGLE, AND WEI ZHENG 2 THE VOLTAGE-GATED ION CHANNEL SUPERFAMILY 7 WILLIAM A. CATTERALL 2.1 INTRODUCTION 7 2.2 VOLTAGE-GATED SODIUM CHANNELS 7 2.3 VOLTAGE-GATED CALCIUM CHANNELS 9 2.4 VOLTAGE-GATED POTASSIUM CHANNELS 11 2.5 INWARDLY RECTIFYING POTASSIUM CHANNELS 12 2.6 COMMON ASPECTS OF ION CHANNEL STRUCTURE AND FUNCTION 13 2.7 CONCLUSIONS 14 3 STATE-DEPENDENT DRUG INTERACTIONS WITH ION CHANNELS 19 STEFAN I. MCDONOUGH AND BRUCE P. BEAN 3.1 INTRODUCTION 19 3.2 ION CHANNELS AS DRUG RECEPTORS 20 3.3 ION CHANNELS ADOPT MULTIPLE CONFORMATIONS 21 3.4 BIOPHYSICS MEETS PHARMACOLOGY: STATE DEPENDENCE, VOLTAGE DEPENDENCE, AND THE MODULATED RECEPTOR MODEL 24 3.5 USE DEPENDENCE 28 3.6 PHYSICAL MEANING OF STATE DEPENDENCE 30 3.7 STATE DEPENDENCE IN DRUG DISCOVERY 31 3.8 FUTURE DIRECTIONS FOR ION CHANNEL DRUG DISCOVERY 33 VOLTAGE-GATED ION CHANNELS AS DRUG TARGETS. EDITED BY D. TRIGGLE COPYRIGHT 2006 WILEY-VCH VERLAG GMBH & CO. KGAA, WEINHEIM ISBN 3-527-31258-7 VI CONTENTS 4 ASSAY TECHNOLOGIES: TECHNIQUES AVAILABLE FOR QUANTIFYING DRUG-CHANNEL INTERACTIONS 37 DEREK LEISHMAN AND GARETH WALDRON 4.1 INTRODUCTION 37 4.2 PATCH CLAMP 39 4.2.1 BASIC DESCRIPTION OF TECHNIQUE 39 4.2.2 ADVANTAGES AND DISADVANTAGES OF MANUAL PATCH CLAMP 42 4.2.3 USE OF PATCH CLAMP FOR QUANTIFICATION OF DRUG-CHANNEL EFFECTS 44 4.2.4 CAVEATS OF INTERPRETATIONS IN PATCH CLAMP 47 4.3 PLANAR PATCH CLAMP 48 4.4 TWO-ELECTRODE VOLTAGE CLAMP (TEVC) OF XENOPUS OOCYTES 50 4.5 MEMBRANE POTENTIAL SENSING DYES 51 4.5.1 BASIC DESCRIPTION OF MEMBRANE POTENTIAL-SENSING DYES 52 4.5.2 ADVANTAGES AND DISADVANTAGES OF MEMBRANE POTENTIAL-SENSING DYES 53 4.6 BINDING 56 4.7 ION FLUX 57 4.7.1 FLUORESCENT INDICATORS OF ION FLUX 57 4.7.2 DIRECT MEASUREMENT OF ION FLUX 58 4.8 WHAT TECHNOLOGIES CANNOT BE USED . YET? 59 4.9 SUMMARY 60 5 CALCIUM CHANNELS 65 5.1 OVERVIEW OF VOLTAGE-GATED CALCIUM CHANNELS 65 CLINTON DOERING AND GERALD ZAMPONI 5.1.1 INTRODUCTION 65 5.1.2 NATIVE AND CLONED CALCIUM CHANNELS: NOMENCLATURE AND CLASSIFICATION 65 5.1.3 DISTRIBUTION OF VGCCS AND THEIR PHYSIOLOGICAL ROLES 66 5.1.4 STRUCTURE OF VGCC A, SUBUNITS 69 5.1.5 VGCC MODULATION 72 5.1.6 VGCCS: CHANNELOPATHIES AND PATHOLOGIES 76 5.1.7 SUMMARY 77 5.2 DRUGS ACTIVE AT T-TYPE CA 2+ CHANNELS 84 THOMAS M. CONNOLLY AND JAMES C. BARROW 5.2.1 INTRODUCTION 84 5.2.2 METHODOLOGY 85 5.2.3 INDICATIONS 92 5.2.4 CONCLUSIONS 94 CONTENTS VII 5.3 L-TYPE CALCIUM CHANNELS 200 DAVID J. TRIGGLE 5.3.1 INTRODUCTION 100 5.3.2 DRUGS THAT INTERACT WITH L-TYPE CHANNELS 100 5.3.3 SPECIFIC DRUG CLASSES 103 5.3.4 OTHER DRUG CLASSES ACTIVE AT CA V L CHANNELS 114 5.3.5 DRUG INTERACTIONS AT NON-A-SUBUNIT SITES 116 5.3.6 CALCIUM ANTAGONISM THROUGH GENE DELIVERY 118 5.4 N-TYPE CALCIUM CHANNELS 122 TERRANCE P. SNUTCH 5.4.1 INTRODUCTION 122 5.4.2 N-TYPE CALCIUM CHANNEL PHARMACOLOGY 123 5.4.3 INORGANIC CATIONS 124 5.4.4 PEPTIDE BLOCKERS 125 5.4.5 SMALL ORGANIC MOLECULE N-TYPE BLOCKERS 132 5.4.6 CONCLUSIONS 140 6 SODIUM CHANNELS 151 6.1 MOLECULAR, BIOPHYSICAL AND FUNCTIONAL PROPERTIES OF VOLTAGE-GATED SODIUM CHANNELS 151 DOUGLAS S. KRAFIE, MARK CHAPMAN, AND KEN MCCORMACK 6.1.1 INTRODUCTION 252 6.1.2 PRIMARY AND TERTIARY STRUCTURE 252 6.1.3 SODIUM CHANNEL EXPRESSION 257 6.1.4 BIOPHYSICAL PROPERTIES OF VOLTAGE-DEPENDENT SODIUM CHANNELS 259 6.1.5 DISEASE ASSOCIATION 262 6.1.6 CONCLUSIONS 265 6.2 SMALL MOLECULE BLOCKERS OF VOLTAGE-GATED SODIUM CHANNELS 168 JESUS E. GONZALEZ, ANDREAS P. TERMIN, AND DEAN M. WILSON 6.2.1 DRUGS THAT ACT ON SODIUM CHANNELS 268 6.2.2 NEW INSIGHTS FOR LAUNCHED COMPOUNDS 270 6.2.3 CHALLENGES OF CURRENT AGENTS 275 6.2.4 COMPOUNDS IN CLINICAL DEVELOPMENT 276 6.2.5 NEW BLOCKERS IN DISCOVERY OR PRE-CLINICAL STAGE 280 6.2.6 EMERGING INDICATIONS AND FUTURE DIRECTIONS 286 VIM CONTENTS 7 POTASSIUM CHANNELS 193 7.1 POTASSIUM CHANNELS: OVERVIEW OF MOLECULAR, BIOPHYSICAL AND PHARMACOLOGICAL PROPERTIES 193 MURALI GOPALAKRISHNAN, CHAR-CHANG SHIEH, AND JUN CHEN 7.1.1 INTRODUCTION 193 7.1.2 CLASSIFICATION AND GENERAL PROPERTIES 194 7.1.3 AUXILIARY SUBUNITS 202 7.1.4 CRYSTAL STRUCTURE 201 7.1.5 K + CHANNELS AND DISEASES 204 7.1.6 LIGANDS INTERACTING WITH K + CHANNELS 204 7.1.7 LIGAND BINDING SITES 206 7.1.8 PEPTIDES AND TOXINS 209 7.1.9 SUMMARY 210 7.2 KVL.3 POTASSIUM CHANNEL: PHYSIOLOGY, PHARMACOLOGY AND THERAPEUTIC INDICATIONS 214 K. GEORGE CHANDY, HEIKE WULFF, CHRISTINE BEETON, PETER A. CALABRESI, GEORGE A. GUTMAN, AND MICHAEL PENNINGTON 7.2.1 INTRODUCTION 214 7.2.2 PEPTIDE INHIBITORS OF KVL.3 216 7.2.3 SMALL MOLECULES INHIBITORS OF KVL.3 222 7.2.4 PHYSIOLOGICAL ROLE OF KVL.3 AND THE EFFECTS OF KVL.3 BLOCKERS 7.2.5 DISEASE INDICATIONS 246 7.2.6 CONCLUSIONS 251 7.3 DRUGS ACTIVE AT KVL.5 POTASSIUM CHANNELS [1] 275 STEFAN PEUKERT AND HEINZ GOGELEIN 7.3.1 STRUCTURE OF THE KVL.5 CHANNEL 275 7.3.2 PHARMACOLOGICAL SIGNIFICANCE OF THE KVL.5 CHANNEL 276 7.3.3 KNOWN DRUGS WITH ACTIVITY ON KVL.5 278 7.3.4 STRUCTURAL CLASSES OF NEW KVL.5 CHANNEL BLOCKERS, THEIR STRUCTURE-ACTIVITY RELATIONSHIP AND PHARMACOLOGY 283 7.3.5 STRATEGIES IN LEAD IDENTIFICATION FOR KVL.5 BLOCKERS 296 7.3.6 SELECTIVITY AGAINST OTHER ION CHANNELS 301 7.3.7 STRUCTURAL BASIS FOR KVL.5 CHANNEL BLOCK 302 7.4 MEDICINAL CHEMISTRY OF CA 2+ -ACTIVATED K + CHANNEL MODULATORS SEAN C. TURNER AND CHAR-CHANG SHIEH 7 A.I INTRODUCTION 310 7.4.2 MEDICINAL CHEMISTRY 318 7.4.3 CONCLUSIONS 329 231 310 7.5 7.5.1 7.5.2 7.5.3 7.5.4 7.5.5 7.5.6 7.5.7 7.6 7.6.1 7.6.2 7.6.3 7.6.4 7.6.5 7.6.6 7.6.7 7.6.8 7.6.9 7.6.10 7.6.11 7.6.12 8 8.1 8.1.1 8.1.2 8.1.3 8.1.4 8.1.5 8.1.6 8.1.7 8.1.8 8.1.9 8.1.10 CONTENTS IX DRUGS ACTIVE AT ATP-SENSITIVE K + CHANNELS 335 WILLIAM A. CARROLL INTRODUCTION 335 MITOCHONDRIAL K ATP CHANNEL OPENERS FOR MYOCARDIAL ISCHEMIA 337 SARC-K ATP BLOCKERS FOR VENTRICULAR ARRHYTHMIA 339 SUR1/KIR6.2 OPENERS FOR DIABETES AND HYPERINSULINEMIA 340 SUR2B/KIR6.2 OPENERS FOR OVERACTIVE BLADDER (OAB) 343 K ATP OPENERS FOR ALOPECIA 348 CONCLUSIONS 348 COMPOUNDS THAT ACTIVATE KCNQ(2-5) FAMILY OF POTASSIUM ION CHANNELS 355 GRANT MCNAUGHTON-SMITH AND ALAN D. WICKENDEN INTRODUCTION 355 FLUPIRTINE, RETIGABINE AND RELATED COMPOUNDS 355 BENZANILIDE, BENZISOXAZOLE AND INDAZOLE DERIVATIVES 360 OXINDOLES AND QUINOLINONES 362 2,4-DISUBSTITUTED PYRIMIDINE-5-CARBOXAMIDES DERIVATIVES 364 CINNAMIDE DERIVATIVES AND ANALOGUES 365 5-CARBOXAMIDE-THIAZOLE DERIVATIVES 370 BENZOTHIAZOLES AS KCNQ(2-5) AGONISTS 372 QUINAZOLINONES DERIVATIVES 373 SALICYLIC ACID DERIVATIVES 375 MELCOFENAMIC ACID AND DICLOFENAC-BASED KCNQ(2-5) AGONISTS 375 SUMMARY 377 GENETIC AND ACQUIRED CHANNELOPATHIES 381 INHERITED DISORDERS OF ION CHANNELS 381 KATE BRACEY AND DENNIS WRAY INTRODUCTION 381 POTASSIUM CHANNELS 383 NON-SELECTIVE CATION CHANNELS 390 TRANSIENT RECEPTOR POTENTIAL (TRP) CHANNELS 392 VOLTAGE-GATED SODIUM CHANNELS 393 NONVOLTAGE-GATED SODIUM CHANNELS 397 CALCIUM CHANNELS 399 CHLORIDE CHANNELS 403 LIGAND-GATED CHANNELS 408 CONCLUSIONS 412 CONTENTS 8.2 STRUCTURAL AND LIGAND-BASED MODELS FOR HERG AND THEIR APPLICATION IN MEDICINAL CHEMISTRY 428 YI LI, GIOVANNI CIANCHETTA, AND ROY J. VAZ 8.2.1 INTRODUCTION: PERSPECTIVE ON THE NECESSITY OF MODELS 428 8.2.2 STRUCTURAL ASPECT OF HERG MODELS 430 8.2.3 LIGAND-BASED CHEMOMETRIC MODELS 430 8.2.4 LIGAND-BASED QSAR MODELS 434 8.2.5 APPLICATION OF MODELS TO IMPROVE SELECTIVITY: CASE STUDIES 434 8.2.6 CONCLUSIONS 440 8.3 ION CHANNEL SAFETY ISSUES IN DRUG DEVELOPMENT 444 ARMANDO A. LAGRUTTA AND JOSEPH J.' SALATA 8.3.1 INTRODUCTION 444 8.3.2 REGULATORY-INDUSTRY RELATIONSHIP (ICH); SAFETY PHARMACOLOGY 444 8.3.3 SAFETY ISSUES SPECIFIC TO THE HERG CHANNEL 449 8.3.4 "INTEGRATED RISK ASSESSMENT" OF DELAYED VENTRICULAR REPOLARIZATION 455 8.3.5 BEYOND QT PROLONGATION 457 8.3.6 ISSUES SPECIFIC TO ION CHANNEL TARGETS 459 INDEX 467
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dewey-sort	3571.64
dewey-tens	570 - Biology 610 - Medicine and health
discipline	Chemie / Pharmazie Biologie Medizin
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format	Book
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institution	BVB
isbn	9783527312580 3527312587
language	English
oai_aleph_id	oai:aleph.bib-bvb.de:BVB01-014865553
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physical	XII, 479 S. Ill., graph. Darst. 25 cm
publishDate	2006
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publisher	Wiley-VCH-Verl.
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series	Methods and principles in medicinal chemistry
series2	Methods and principles in medicinal chemistry
spelling	Voltage-gated ion channels as drug targets ed. by David J. Triggle ... Weinheim Wiley-VCH-Verl. 2006 XII, 479 S. Ill., graph. Darst. 25 cm txt rdacontent n rdamedia nc rdacarrier Methods and principles in medicinal chemistry 29 Literaturangaben Canaux ioniques Membranes (Biologie) Drug Delivery Systems Drug Design Ion Channels Ion channels Membranes (Biology) Spannungskontrollierter Ionenkanal (DE-588)4717815-2 gnd rswk-swf Targeted drug delivery (DE-588)4302415-4 gnd rswk-swf (DE-588)4143413-4 Aufsatzsammlung gnd-content Spannungskontrollierter Ionenkanal (DE-588)4717815-2 s Targeted drug delivery (DE-588)4302415-4 s DE-604 Triggle, David J. (DE-588)131346377 edt Methods and principles in medicinal chemistry 29 (DE-604)BV035418617 29 text/html http://deposit.dnb.de/cgi-bin/dokserv?id=2686576&prov=M&dok_var=1&dok_ext=htm Inhaltstext GBV Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=014865553&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis
spellingShingle	Voltage-gated ion channels as drug targets Methods and principles in medicinal chemistry Canaux ioniques Membranes (Biologie) Drug Delivery Systems Drug Design Ion Channels Ion channels Membranes (Biology) Spannungskontrollierter Ionenkanal (DE-588)4717815-2 gnd Targeted drug delivery (DE-588)4302415-4 gnd
subject_GND	(DE-588)4717815-2 (DE-588)4302415-4 (DE-588)4143413-4
title	Voltage-gated ion channels as drug targets
title_auth	Voltage-gated ion channels as drug targets
title_exact_search	Voltage-gated ion channels as drug targets
title_exact_search_txtP	Voltage-gated ion channels as drug targets
title_full	Voltage-gated ion channels as drug targets ed. by David J. Triggle ...
title_fullStr	Voltage-gated ion channels as drug targets ed. by David J. Triggle ...
title_full_unstemmed	Voltage-gated ion channels as drug targets ed. by David J. Triggle ...
title_short	Voltage-gated ion channels as drug targets
title_sort	voltage gated ion channels as drug targets
topic	Canaux ioniques Membranes (Biologie) Drug Delivery Systems Drug Design Ion Channels Ion channels Membranes (Biology) Spannungskontrollierter Ionenkanal (DE-588)4717815-2 gnd Targeted drug delivery (DE-588)4302415-4 gnd
topic_facet	Canaux ioniques Membranes (Biologie) Drug Delivery Systems Drug Design Ion Channels Ion channels Membranes (Biology) Spannungskontrollierter Ionenkanal Targeted drug delivery Aufsatzsammlung
url	http://deposit.dnb.de/cgi-bin/dokserv?id=2686576&prov=M&dok_var=1&dok_ext=htm http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=014865553&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA
volume_link	(DE-604)BV035418617
work_keys_str_mv	AT triggledavidj voltagegatedionchannelsasdrugtargets

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