Glutamate and GABA receptors and transporters: structure, function and pharmacology
Saved in:
| Format: | Book |
|---|---|
| Language: | English |
| Published: |
London [u.a.]
Taylor & Francis
2002
|
| Edition: | 1. publ. |
| Series: | The Taylor & Francis series in pharmaceutical sciences
|
| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Physical Description: | XII, 435 S. Ill., graph. Darst. |
| ISBN: | 0748408819 |
Staff View
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| 245 | 1 | 0 | |a Glutamate and GABA receptors and transporters |b structure, function and pharmacology |c ed. by Jan Egebjerg ... |
| 250 | |a 1. publ. | ||
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Record in the Search Index
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| adam_text | Contents
List of contributors xi
PART 1
lonotropic glutamate receptors I
1 lonotropic glutamate receptors: functional and pharmacological
properties in relation to constituent subunits 3
STUART G. CULL CANDY
Introduction 3
Classes of ionotropic glutamate receptors, subunits and assemblies 3
Pharmacological properties of AMP A and kainate Rs 11
Functional diversity ofnon NMDARs 14
Pharmacological and functional characteristics ofNMDARs 21
NMDAR diversity 26
Concluding remarks 29
2 Structure of ionotropic glutamate receptors 41
JAN EGEBJERG AND HENRIK S. JENSEN
Evolution of ionotropic glutamate receptors 41
Assembly of ionotropic glutamate receptors 43
The pore region 49
3 Glutamate receptor trafficking 56
GUIDO MEYER AND JEREMY M. HENLEY
Introduction 56
Proteins interacting with NMDA receptors 56
Proteins interacting with AMPA receptors 60
Concluding remarks 63
vi Contents 4 Pharmacology of NMDA receptors 69
DAVID JANE
Introduction 69
Agonists interacting with the glutamate binding site 10
Competitive NMDA receptor antagonists 73
Pharmacophore modelling of competitive NMDA receptor antagonists 78
Subtype selectivity of competitive NMDA receptor antagonists 79
Ligands binding to the glycine co agonist site of the NMDA receptor 80
Channel blocking uncompetitive NMDA receptor antagonists 84
Non competitive NMDA receptor antagonists 86
Concluding remarks 89
5 Pharmacology of AMPA/kainate receptors 99
ULF MADSEN, TOMMY N. JOHANSEN, TINE B. STENSB0L AND
POVL KROGSGAARD LARSEN
Introduction 99
Naturally occurring AMPA/kainate receptor agonists 99
Ibotenic acid as a lead structure 101
AMP A receptor agonists 102
AMP A receptor antagonists 106
AMP A receptor modulators 109
Kainatereceptors 111
Conclusion 113
PART 2
Metabotropic glutamate receptors 119
6 Metabotropic glutamate receptors (mGluRs): structure
and function 121
J. BOCKAERT, L. FAGNI AND J. P. PIN
Introduction and general presentation 121
mGluRs are members of family 3 GPCRs 122
Tlie binding domain ofmGluRs 123
TlieTMDofmGluRs 126
Activation and coupling to G proteins 126
Transdudion mechanisms 129
Roles ofmGluRs in synoptic transmission 134
Pathologies which may benefit from specific drugs acting on mGluRs 137
Conclusion 142
Contents vii
7 Pharmacology of metabotropic glutamate receptors 151
DARRYLE D. SCHOEPP AND JAMES A. MONN
Background 151
Agonist pharmacology 152
Antagonist pharmacology 164
Past/future perspectives 116
PART 3
GABAA receptors 187
8 Insights into GABAA receptor complexity from the study of
cerebellar granule cells: synaptic and extrasynaptic receptors 189
WILLIAM WISDEN AND MARK FARRANT
Introduction 189
The cerebellum 189
The GABAergic inhibition of granule cells 190
Assembly rules for GABAA receptor submits 191
GABAA receptor expression during granule cell development 193
Differential subcellular targeting of GABAA receptors 195
Other brain regions which use a.68 and a48 containing receptors 196
Evolution and redundancy of the a6 system 191
Conclusions 191
9 GABAA receptor complex: structure and function 202
RICHARD W. OLSEN AND ROBERT L. MACDONALD
Introduction 202
Native receptors 203
Functional domains for assembly, targeting, and trafficking 206
Phosphorylation substrates and functional correlates 209
Functional domains involved in the ion channel 212
Functional domains for agonist and allosteric drug actions 216
10 Ligands for the GABAA receptor complex 236
POVL KROGSGAARD LARSEN, BENTE FR0LUND, UFFE KRISTIANSEN AND
BJARKE EBERT
GABA inhibition and disinhibition 236
GABA in the peripheral nervous system: transmitter andparacrine effector 236
GABA receptors 239
GABAA agonists 251
GABAA antagonists 258
Partial GABAA agonists 259
Future challenges 263
viii Contents
PART 4
Metabotropic GABA receptors 275
11 Molecular structure of the GABAB receptors 277
N. KXIX AND B. BETTLER
Introduction 277
The GABAB receptor 277
Neurophysiology of GABAB receptor subtypes 280
Spatial and temporal distribution of cloned GABAB receptors 281
Conclusion 282
12 Pharmacology of GABAB receptors 287
N.G. BOWERY
Introduction 287
Functional role ofGABAB receptors in mammals 288
GABAB receptor distribution in CNS 289
GABAB receptor effector mechanisms 291
PART 5
Glutamate and GABA transporters 305
13 Structure, function and regulation of glutamate transporters 307
LINE M. LEVY
Introduction 307
Transmembraneglutamate transport in the CNS 307
Na4 dependentglutamate transporters 309
Concluding remarks 323
14 GABA transporters: functional and pharmacological properties 337
ARNE SCHOUSBOE AND BARUCH KANNER
Introduction 337
Basic properties of GABA transporters 337
Basic pharmacology of cloned transporters 338
Pharmacology ofneuronal andglial GABA transport 340
Molecular studies ofligand binding and transport in GAT 1 341
Regional and cellular localization of GABA carriers 343
Functional and behavioral correlates of GABA transport 343
Regulation of expression and activity of GABA transporters 344
Contents ix
PART 6
Pathophysiology and therapeutic prospects 351
15 Transgenic models for glutamate receptor function 353
AJ. DOHERTY AND G.L. COLLINGRIDGE
Introduction 353
Ionotropic glutamate receptors 356
Metabotropic glutamate receptors 365
Concluding remarks 368
16 Transgenic models for GABAA receptor function 375
H. MOHLER
Introduction 375
Independent regulation of subunit gene transcription 315
Receptor assembly and targeting 316
Anchoring and clustering of GABAA receptors 311
Mechanism of action of drugs acting on QABAA receptors 318
GABA4 receptor mutations and phenotypic pathophysiology 380
From genotype to phenotype 381
17 Glutamatergic transmission: therapeutic prospects for
schizophrenia and Alzheimer s disease 385
NURI B. FARBER, JOHN W. NEWCOMER AND JOHN W. OLNEY
Introduction 385
NRHypo produces brain damage in the rat 386
NRHypo hypothesis of schizophrenia 391
Potential inconsistencies of the NRHypo schizophrenia hypothesis 394
NRHypo hypothesis of AD 395
Comparison of the NRHypo models of schizophrenia and AD 399
Treatment implications 400
Summary 401
18 Modulators of the GABAA receptor: novel therapeutic
prospects 407
CHRISTIAN THOMSEN AND BJARKE EBERT
Introduction 407
Receptor functional considerations for novel modulators of the GABAergic system 408
New subtype selective modulators of the GABAergic system 411
Epilepsy 412
Anxiety disorders 414
Sleep 414
x Contents
Premenstrual dysphoric disorder 411
Analgesia 418
Memory /learning 418
Schizophrenia 419
Stroke 420
Future perspectives 420
Index 429
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| spelling | Glutamate and GABA receptors and transporters structure, function and pharmacology ed. by Jan Egebjerg ... 1. publ. London [u.a.] Taylor & Francis 2002 XII, 435 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier The Taylor & Francis series in pharmaceutical sciences gamma-Aminobutyric Acid cabt Receptors cabt Glutamate Receptors cabt Carrier Proteins Carrier proteins GABA Receptors Glutamic acid Receptors Receptors, GABA physiology Receptors, Glutamate physiology GABA-Rezeptor (DE-588)4280103-5 gnd rswk-swf Metabotroper Glutamatrezeptor (DE-588)4539080-0 gnd rswk-swf Glutamatrezeptor (DE-588)4325632-6 gnd rswk-swf Glutamatrezeptor (DE-588)4325632-6 s DE-604 Metabotroper Glutamatrezeptor (DE-588)4539080-0 s GABA-Rezeptor (DE-588)4280103-5 s Egebjerg, Jan Sonstige oth HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=009745258&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Glutamate and GABA receptors and transporters structure, function and pharmacology gamma-Aminobutyric Acid cabt Receptors cabt Glutamate Receptors cabt Carrier Proteins Carrier proteins GABA Receptors Glutamic acid Receptors Receptors, GABA physiology Receptors, Glutamate physiology GABA-Rezeptor (DE-588)4280103-5 gnd Metabotroper Glutamatrezeptor (DE-588)4539080-0 gnd Glutamatrezeptor (DE-588)4325632-6 gnd |
| subject_GND | (DE-588)4280103-5 (DE-588)4539080-0 (DE-588)4325632-6 |
| title | Glutamate and GABA receptors and transporters structure, function and pharmacology |
| title_auth | Glutamate and GABA receptors and transporters structure, function and pharmacology |
| title_exact_search | Glutamate and GABA receptors and transporters structure, function and pharmacology |
| title_full | Glutamate and GABA receptors and transporters structure, function and pharmacology ed. by Jan Egebjerg ... |
| title_fullStr | Glutamate and GABA receptors and transporters structure, function and pharmacology ed. by Jan Egebjerg ... |
| title_full_unstemmed | Glutamate and GABA receptors and transporters structure, function and pharmacology ed. by Jan Egebjerg ... |
| title_short | Glutamate and GABA receptors and transporters |
| title_sort | glutamate and gaba receptors and transporters structure function and pharmacology |
| title_sub | structure, function and pharmacology |
| topic | gamma-Aminobutyric Acid cabt Receptors cabt Glutamate Receptors cabt Carrier Proteins Carrier proteins GABA Receptors Glutamic acid Receptors Receptors, GABA physiology Receptors, Glutamate physiology GABA-Rezeptor (DE-588)4280103-5 gnd Metabotroper Glutamatrezeptor (DE-588)4539080-0 gnd Glutamatrezeptor (DE-588)4325632-6 gnd |
| topic_facet | gamma-Aminobutyric Acid Receptors Glutamate Receptors Carrier Proteins Carrier proteins GABA Receptors Glutamic acid Receptors Receptors, GABA physiology Receptors, Glutamate physiology GABA-Rezeptor Metabotroper Glutamatrezeptor Glutamatrezeptor |
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