The muscarinic receptors
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| Format: | Buch |
|---|---|
| Sprache: | English |
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Clifton, NJ
Humana Press
1989
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| Schriftenreihe: | The receptors
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| 245 | 1 | 0 | |a The muscarinic receptors |c ed. by Joan Heller Brown |
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| adam_text | THE MUSCARINIC RECEPTORS EDITED BY JOAN HELLER BROWN UNIVERSITY OF
CALIFORNIA, SAN DIEGO LA JOLLA, CALIFORNIA THE HUMANA PRESS * CLIFTON,
NEW JERSEY CONTENTS PREFACE V LIST OF CONTRIBUTORS XVII SECTION 1:
HISTORICAL PERSPECTIVES CHAPTER 1 HISTORY AND BASIC PROPERTIES OF THE
MUSCARINIC CHOLINERGIC RECEPTORS A. S. V. BURGEN 1. HISTORY 3 2. THE
RANGE OF MUSCARINIC ACTIVITY 7 3. MUSCARINIC AGONISTS 10 4. MUSCARINIC
ANTAGONISTS 10 5. RECEPTOR BINDING STUDIES 11 6. QUANTITATION OF
MUSCARINIC EFFECTS IN INTACT TISSUES 16 7. PHYSIOLOGICAL AND BIOCHEMICAL
ACTIONS OF MUSCARINIC AGONISTS 18 7.1. ACTIONS THROUGH ADENYLATE CYCLASE
18 7.2. ACTIONS THROUGH INOSITOL PHOSPHATES 19 7.3. ACTIONS ON POTASSIUM
PERMEABILITY .... V 19 7.4. ACTIONS ON CALCIUM PERMEABILITY 19 8.
SUBTYPES OF THE MUSCARINIC RECEPTOR 20 REFERENCES 22 SECTION 2:
PHARMACOLOGICAL PROPERTIES, PURIFICATION, AND CLONING OF MUSCARINIC
RECEPTORS CHAPTER 2 THE BINDING PROPERTIES OF MUSCARINIC RECEPTORS N. J.
M. BIRDSALL AND E. C. HULME 1. INTRODUCTION 31 OII VIII CONTENTS 2. THE
BINDING OF ANTAGONISTS 32 2.1. EARLY STUDIES: A SIMPLE PICTURE 32 2.2.
RECENT STUDIES: A VERY COMPLEX PICTURE 33 2.3. COMPARISON OF THE BINDING
PROPERTIES OF RECEPTORS IN DIFFERENT TISSUES 35 2.4. SIMPLIFICATION OF
THE BINDING PATTERN BY THE USE OF TRITIATED SELECTIVE ANTAGONISTS 37
2.5. SIMPLIFICATION AND ANALYSIS OF THE BINDING COMPLEXITY BY TAKING
ADVANTAGE OF THE DIFFERENT KINETICS OF [ 3 H]NMS BINDING TO THE RECEPTOR
SUBCLASSES 39 2.6. EFFECTS OF INCUBATION CONDITIONS ON ANTAGONIST
BINDING 42 2.7. DRUGS THAT DO NOT BIND AT THE SAME SITE AS ACETYLCHOLINE
OR ATROPINE 44 2.8. SOLUBLE RECEPTORS 46 2.9. DIFFERENCES IN THE BINDING
OF HYDROPHOBIC AND HYDROPHILIC LIGANDS TO MUSCARINIC RECEPTORS 50 2.10.
BINDING STUDIES ON SMOOTH MUSCLE 55 3. THE BINDING OF AGONISTS 56 3.1.
EARLY STUDIES 56 3.2. SIMPLIFICATION OF THE AGONIST BINDING PROPERTIES
59 3.3. MODULATION OF THE AGONIST BINDING PROPERTIES BY DIVALENT CATIONS
AND NUCLEOTIDES 62 3.4. MODELS FOR AGONIST BINDING HETEROGENEITY ... 65
3.5. MODULATION OF THE AGONIST BINDING PROPERTIES BY OTHER AGENTS *. 68
3.6. SOLUBLE RECEPTORS 72 4. GENERAL CONCLUSIONS 73 REFERENCES 74
CHAPTER 3 MUSCARINIC RECEPTOR PURIFICATION AND PROPERTIES MICHAEL
SCHIMERLIK 1. SOLUBILIZATION AND PURIFICATION OF MUSCARINIC RECEPTORS 93
1.1. SOLUBILIZATION OF MUSCARINIC RECEPTORS (MACHR) 93 1.2. PURIFICATION
OF MUSCARINIC RECEPTORS 95 CONTENTS IX 2. LIGAND BINDING PROPERTIES OF
PURIFIED MUSCARINIC RECEPTORS 96 3. PHYSICAL PROPERTIES AND STRUCTURAL
STUDIES OF MUSCARINIC RECEPTORS 97 3.1. GLYCOPROTEIN PROPERTIES 97 3.2.
PHYSICAL PROPERTIES 99 4. CLONING OF MUSCARINIC RECEPTORS 103 4.1.
AMINO-ACID SEQUENCE AND STRUCTURE DEDUCED FROM CDNA CLONES 103 4.2.
RECEPTOR EXPRESSION 109 5. RECONSTITUTION OF MUSCARINIC RECEPTORS WITH
GUANINE NUCLEOTIDE BINDING PROTEINS 112 REFERENCES 117 CHAPTER 4
SUBTYPES OF MUSCARINIC CHOLINERGIC RECEPTORS: LIGAND BINDING, FUNCTIONAL
STUDIES, AND CLONING BARRY B. WOLFE 1. INTRODUCTION 125 2. PHYSIOLOGICAL
STUDIES 126 3. RADIOLIGAND BINDING STUDIES 130 4. MOLECULAR CLONING OF
GENES FOR MUSCARINIC RECEPTORS 139 5. CONCLUSIONS 144 REFERENCES 144
CHAPTER 5 STRUCTURAL DETERMINANTS OF MUSCARINIC AGONIST ACTIVITY BJORN
RINGDAHL 1. INTRODUCTION 151 2. ANALOGS OF ACETYLCHOLINE 154 2.1.
CONFORMATIONALLY RESTRICTED ANALOGS OF ACETYLCHOLINE 154 2.2. AFFINITY
AND EFFICACY OF ACETYLCHOLINE ANALOGS 158 2.3. MOLECULAR MODELS FOR
ACETYLCHOLINE-LIKE LIGANDS 161 3. ANALOGS OF MUSCARINE 162 3.1.
CYCLOPENTANE AND CYCLOPENTENE DERIVATIVES . 163 CONTENTS 3.2.
TETRAHYDROFURANE AND TETRAHYDROTHIOPHENE DERIVATIVES 165 3.3.
OXATHIOLANES 166 3.4. AFFINITY AND EFFICACY OF MUSCARINE ANALOGS .. 167
4. ANALOGS OF ARECOLINE 168 4.1. TETRAHYDROPYRIDINE ANALOGS 169 4.2.
DIHYDROTHIOPYRANES 170 4.3. 3-PYRROLINE DERIVATIVES 171 4.4.
CONFORMATIONALLY RESTRICTED TETRAHYDROPYRIDINE DERIVATIVES 172 5.
ANALOGS OF OXOTREMORINE 173 5.1. STRUCTURE-AFFINITY AND
STRUCTURE-EFFICACY RELATIONSHIPS 173 5.2. RELATIONSHIP BETWEEN AFFINITY
AND EFFICACY AND BIOCHEMICALLY DETERMINED DRUG PARAMETERS . 188 5.3.
SELECTIVITY OF PARTIAL AGONISTS 189 6. ATYPICAL MUSCARINIC AGONISTS 195
6.1. ANALOGS OF MCN-A-343 195 6.2. ANALOGS OF RS 86 197 6.3. ANALOGS OF
PILOCARPINE 197 6.4. ANALOGS OF AF 30 198 7. HALOALKYLAMINE DERIVATIVES
OF MUSCARINIC AGONISTS 199 7.1. ANALOGS OF ACETYLCHOLINE 200 7.2.
ANALOGS OF OXOTREMORINE 200 REFERENCES 205 SECTION 3: BIOCHEMICAL
EFFECTORS COUPLED TO MUSCARINIC RECEPTORS CHAPTER 6 MUSCARINIC
CHOLINERGIC RECEPTOR-MEDIATED REGULATION OF CYCLIC AMP METABOLISM T.
KENDALL HARDEN 1. INTRODUCTION 221 2. REGULATION OF CYCLIC AMP SYNTHESIS
222 2.1. GENERAL MODEL FOR ACTIVATION OF ADENYLATE CYCLASE 222 2.2.
RECEPTOR-MEDIATED INHIBITION OF ADENYLATE CYCLASE 224 CONTENTS XI 2.3.
OBSERVATIONS ON MACHR-MEDIATED INHIBITION OF ADENYLATE CYCLASE 229 3.
RECEPTOR-MEDIATED ACTIVATION OF PHOSPHODIESTERASE 232 3.1. GENERAL
PROPERTIES 232 3.2. PHOSPHODIESTERASE IN THYROID SLICES 233 3.3.
PHOSPHODIESTERASE IN ASTROCYTOMA CELLS 234 3.4. MECHANISM OF ACTIVATION
OF PHOSPHODIESTERASE 235 4. COMPARATIVE PROPERTIES OF THE TWO SECOND-
MESSENGER RESPONSE SYSTEMS INVOLVED IN MACHR-MEDIATED LOWERING OF CYCLIC
AMP LEVELS 242 5. CONCLUSIONS . 246 REFERENCES 247 CHAPTER 7 MUSCARINIC
CHOLINERGIC RECEPTOR REGULATION OF INOSITOL PHOSPHOLIPID METABOLISM AND
CALCIUM MOBILIZATION JOAN HELLER BROWN AND PATRICK M. MCDONOUGH 1. THE
PHOSPHOINOSITIDE CYCLE 259 2. TISSUE LOCALIZATION OF MUSCARINIC
RECEPTOR- STIMULATED INOSITOL PHOSPHOLIPID HYDROLYSIS 262 3.
RELATIONSHIP BETWEEN AGONIST OCCUPANCY AND THE PHOSPHOINOSITIDE RESPONSE
266 4. DIFFERENTIAL EFFECTS OF MUSCARINIC AGONISTS ON PHOSPHOINOSITIDE
HYDROLYSIS 269 5. RELATIONSHIP OF MUSCARINIC RECEPTOR SUBTYPES TO THE
REGULATION OF PHOSPHOLIPASE C 271 6. EVIDENCE THAT A GTP-BINDING PROTEIN
TRANSDUCES MUSCARINIC RECEPTOR BINDING INTO ACTIVATION OF PHOSPHOLIPASE
C 274 7. REGULATION OF MUSCARINIC RECEPTOR-MEDIATED PHOSPHOINOSITIDE
HYDROLYSIS BY PROTEIN KINASE C . 278 8. MUSCARINIC RECEPTOR STIMULATION
OF CALCIUM MOBILIZATION ..280 9. THE ROLE OF INOSITOL TRISPHOSPHATE IN
RELEASE OF CALCIUM FROM INTRACELLULAR STORES 284 10. DEPLETION AND
REFILLING OF CALCIUM STORES 286 11. ROLE OF CALCIUM ELEVATION IN
MUSCARINIC RESPONSES 287 12. CONCLUSIONS AND FUTURE DIRECTIONS 288
REFERENCES 289 XII CONTENTS CHAPTER 8 MUSCARINIC RECEPTOR REGULATION OF
CYCLIC GMP AND EICOSANOID PRODUCTION MICHAEL MCKINNEY AND ELLIOTT
RICHELSON 1. PHYSIOLOGY 309 1.1. MUSCARINIC RECEPTOR-MEDIATED CYCLIC GMP
FORMATION IN CELLS 309 1.2. FUNCTION OF CYCLIC GMP IN VARIOUS SYSTEMS .
310 2. MUSCARINIC RECEPTOR SUBTYPE MEDIATING CYCLIC GMP FORMATION .315
2.1. N1E-115 NEUROBLASTOMA CELLS 315 2.2. CORRELATION OF CYCLIC GMP AND
PHOSPHOINOSITIDE METABOLISM 317 3. POSSIBLE MECHANISMS OF ACTIVATION OF
GUANYLATE CYCLASE 318 3.1. CALCIUM CHANNELS 318 3.2. OXYGEN AND LIPIDS
320 4. MUSCARINIC RECEPTOR-MEDIATED ARACHIDONATE METABOLISM 323 4.1.
BLOCKADE OF MUSCARINIC RESPONSES BY ARACHIDONIC METABOLIC INHIBITORS 323
4.2. RELEASE OF EICOSANOIDS BY THE MUSCARINIC RECEPTOR 324 4.3.
LIPOXYGENATION IN NEURAL TISSUE AND RELEVANCE TO DISEASE 326 REFERENCES
327 CHAPTER 9 MUSCARINIC CHOLINERGIC RECEPTOR REGULATION OF ION
CHANNELS R. ALAN NORTH 1. INTRODUCTION 341 2. POTASSIUM CONDUCTANCE
INCREASE 343 2.1. HEART ...343 2.2. NEURONS 346 2.3. GLANDS 348 2.4.
OOCYTES 349 3. POTASSIUM CONDUCTANCE DECREASE 349 3.1. NEURONS 349 3.2.
SMOOTH MUSCLE 355 4. CALCIUM CHANNELS 355 CONTENTS XIII 4.1. HEART 355
4.2. NEURONS 357 4.3. SMOOTH MUSCLE 358 5. INWARD CURRENTS FROM
INCREASED CATION CONDUCTANCE 358 5.1. HEART 358 5.2. NEURONS 359 5.3.
SMOOTH MUSCLE 359 5.4. GLAND CELLS 360 5.5. OOCYTES 360 6. CHLORIDE
CHANNELS 361 6.1. NEURONS 361 6.2. GLAND CELLS 361 6.3. OOCYTES 361 7.
CONCLUSIONS 362 REFERENCES 364 SECTION 4: REGULATION OF MUSCARINIC
RECEPTORS CHAPTER 10 ALLOSTERIC INTERACTIONS OF MUSCARINIC RECEPTORS AND
THEIR REGULATION BY OTHER MEMBRANE PROTEINS YOAV I. HENIS, YOEL KLOOG,
AND MORDECHAI SOKOLOVSKY 1. ALLOSTERY AND COOPERATIVITY: DEFINITIONS AND
EXPERIMENTAL TOOLS 377 1.1. DEFINITIONS 377 1.2. EXPERIMENTAL TOOLS :
378 2. HOMOTROPIC SITE-SITE INTERACTIONS AMONG MUSCARINIC RECEPTORS
... 381 2.1. IDENTIFICATION OF COOPERATIVE INTERACTIONS BETWEEN
MUSCARINIC BINDING SITES IN RAT ADENOHYPOPHYSIS USING COMPETITION
STUDIES 381 2.2. STUDIES ON SITE-SITE INTERACTIONS IN HEART AND BRAIN
MUSCARINIC RECEPTORS 384 3. ALLOSTERIC INTERACTIONS OF MUSCARINIC
RECEPTORS 386 3.1. INTERACTIONS OF GALLAMINE WITH MUSCARINIC RECEPTORS
386 3.2. BISQUATERNARY PYRIDINIUM OXIMES AS ALLOSTERIC INHIBITORS OF RAT
BRAIN MUSCARINIC RECEPTORS 390 XIO CONTENTS 3.3. ALLOSTERIC INTERACTIONS
OF OTHER DRUGS WITH MUSCARINIC RECEPTORS 395 4. INTERACTION BETWEEN
MUSCARINIC RECEPTORS AND G-PROTEINS 400 5. INTERACTION BETWEEN
MUSCARINIC RECEPTORS AND ION CHANNELS 406 REFERENCES 410 CHAPTER 11
REGULATION AND DEVELOPMENT OF MUSCARINIC RECEPTOR NUMBER AND FUNCTION
NEIL M. NATHANSON 1. INTRODUCTION 419 2. REGULATION BY EXPOSURE TO
AGONIST 419 2.1. REGULATION OF MACHR NUMBER AND FUNCTION IN CELL CULTURE
420 2.2. REGULATION OF MACHR BY IN VIVO AGONIST AND ANTAGONIST
ADMINISTRATION 422 2.3. RAPID AGONIST-MEDIATED DESENSITIZATION OF
RECEPTOR FUNCTION 423 3. PHYSIOLOGICAL AND BIOCHEMICAL PROPERTIES OF
NEWLY SYNTHESIZED RECEPTORS 425 4. REGULATION BY INNERVATION, HORMONES,
AND FACTORS 427 5. REGULATION BY ELECTRICAL ACTIVITY 431 6. POSSIBLE
ROLES OF PHOSPHORYLATION IN RECEPTOR REGULATION 433 7. DEVELOPMENTAL
CHANGES IN MACHR NUMBERS AND FUNCTION .. 436 7.1. DEVELOPMENTAL CHANGES
IN THE MACHR IN THE CENTRAL NERVOUS SYSTEM 436 7.2. DEVELOPMENTAL
CHANGES IN AND REGULATION OF CARDIAC MACHR 438 8. CONCLUSIONS 442
REFERENCES 443 CONTENTS XV SECTION 5: FUTURE DIRECTIONS CHAPTER 12
FUTURE DIRECTIONS N. J. M. BIRDSALL AND E. C. HULME 1. FUTURE DIRECTIONS
457 REFERENCES 466 INDEX 473
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| genre | (DE-588)4143413-4 Aufsatzsammlung gnd-content |
| genre_facet | Aufsatzsammlung |
| id | DE-604.BV002647134 |
| illustrated | Not Illustrated |
| indexdate | 2025-02-03T16:12:11Z |
| institution | BVB |
| isbn | 089603156X |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-001698441 |
| oclc_num | 20016953 |
| open_access_boolean | |
| owner | DE-12 DE-19 DE-BY-UBM DE-355 DE-BY-UBR |
| owner_facet | DE-12 DE-19 DE-BY-UBM DE-355 DE-BY-UBR |
| physical | XVIII, 478 S. |
| publishDate | 1989 |
| publishDateSearch | 1989 |
| publishDateSort | 1989 |
| publisher | Humana Press |
| record_format | marc |
| series2 | The receptors |
| spellingShingle | The muscarinic receptors Colinergicos e anticolinerg (farmacologia) larpcal Récepteurs muscariniques Muscarinic receptors Receptors, Muscarinic Biochemie (DE-588)4006777-4 gnd Muscarinrezeptor (DE-588)4170773-4 gnd |
| subject_GND | (DE-588)4006777-4 (DE-588)4170773-4 (DE-588)4143413-4 |
| title | The muscarinic receptors |
| title_auth | The muscarinic receptors |
| title_exact_search | The muscarinic receptors |
| title_full | The muscarinic receptors ed. by Joan Heller Brown |
| title_fullStr | The muscarinic receptors ed. by Joan Heller Brown |
| title_full_unstemmed | The muscarinic receptors ed. by Joan Heller Brown |
| title_short | The muscarinic receptors |
| title_sort | the muscarinic receptors |
| topic | Colinergicos e anticolinerg (farmacologia) larpcal Récepteurs muscariniques Muscarinic receptors Receptors, Muscarinic Biochemie (DE-588)4006777-4 gnd Muscarinrezeptor (DE-588)4170773-4 gnd |
| topic_facet | Colinergicos e anticolinerg (farmacologia) Récepteurs muscariniques Muscarinic receptors Receptors, Muscarinic Biochemie Muscarinrezeptor Aufsatzsammlung |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=001698441&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
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