Voltage-gated ion channels as drug targets:
Gespeichert in:
| Weitere Verfasser: | |
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| Format: | Buch |
| Sprache: | English |
| Veröffentlicht: |
Weinheim
Wiley-VCH-Verl.
2006
|
| Schriftenreihe: | Methods and principles in medicinal chemistry
29 |
| Schlagworte: | |
| Online-Zugang: | Inhaltstext Inhaltsverzeichnis |
| Beschreibung: | Literaturangaben |
| Beschreibung: | XII, 479 S. Ill., graph. Darst. 25 cm |
| ISBN: | 9783527312580 3527312587 |
Internformat
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| 245 | 1 | 0 | |a Voltage-gated ion channels as drug targets |c ed. by David J. Triggle ... |
| 264 | 1 | |a Weinheim |b Wiley-VCH-Verl. |c 2006 | |
| 300 | |a XII, 479 S. |b Ill., graph. Darst. |c 25 cm | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 490 | 1 | |a Methods and principles in medicinal chemistry |v 29 | |
| 500 | |a Literaturangaben | ||
| 650 | 4 | |a Canaux ioniques | |
| 650 | 4 | |a Membranes (Biologie) | |
| 650 | 4 | |a Drug Delivery Systems | |
| 650 | 4 | |a Drug Design | |
| 650 | 4 | |a Ion Channels | |
| 650 | 4 | |a Ion channels | |
| 650 | 4 | |a Membranes (Biology) | |
| 650 | 0 | 7 | |a Spannungskontrollierter Ionenkanal |0 (DE-588)4717815-2 |2 gnd |9 rswk-swf |
| 650 | 0 | 7 | |a Targeted drug delivery |0 (DE-588)4302415-4 |2 gnd |9 rswk-swf |
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Datensatz im Suchindex
| _version_ | 1804135457319026688 |
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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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| callnumber-label | QH603 |
| callnumber-raw | QH603.I54 |
| callnumber-search | QH603.I54 |
| callnumber-sort | QH 3603 I54 |
| callnumber-subject | QH - Natural History and Biology |
| classification_rvk | VS 5350 |
| ctrlnum | (OCoLC)64399390 (DE-599)BVBBV021650873 |
| dewey-full | 571.64 610 570 |
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| discipline | Chemie / Pharmazie Biologie Medizin |
| discipline_str_mv | Chemie / Pharmazie Biologie Medizin |
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| index_date | 2024-07-02T15:02:57Z |
| indexdate | 2024-07-09T20:40:48Z |
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| series | Methods and principles in medicinal chemistry |
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| 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 |
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