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Cell surface receptors : a short course on theory & methods / by Lee E. Limbird. — 3rd ed. — New York : Springer Science+Business Media, c2005.—(58.155/L733/3rd ed.)

Contents

        CONTENTS
    
1. INTRODUCTION TO RECEPTOR THEORY 1
ORIGIN OF THE RECEPTOR CONCEPT 2
OCCUPANCY THEORY 7
RELATIONSHIP BETWEEN OCCUPANCY AND RESPONSE 8
CONCEPT OF SPARE RECEPTORS 13
OPERATIONAL MODELS OF PHARMACOLOGICAL AGONISM 14
RATE THEORY 17
ALLOSTERIC THEORY 19
BEYOND TWO-STATE RECEPTOR THEORY 21
SUMMARY 24
2. CHARACTERIZATION OF RECEPTORS BASED ON RECEPTOR-MEDIATED RESPONSES 29
CHARACTERIZATION OF RECEPTOR SPECIFICITY 29
DETERMINING EQUILIBRIUM DISSOCIATION CONSTANTS (KDVALUES) FOR RECEPTOR-LIGAND INTERACTIONS BASED ON MEASUREMENTS OF RECEPTOR-MEDIATED RESPONSE 36
PHARMACOLOGIC RESULTANT ANALYSIS 56
SUMMARY 61
3. IDENTIFICATION OF RECEPTORS USING DIRECT RADIOLIGAND BINDING TECHNIQUES 65
METHODS--DATA GENERATION 65
CRITERIA EXPECTED FOR BINDING OF *D TO THE PHYSIOLOGICALLY RELEVANT RECEPTOR, R 74
DETERMINATION OF RATE CONSTANTS FOR RADIOLIGAND ASSOCIATION AND DISSOCIATION 107
SUMMARY 117
4. COMPLEX BINDING PHENOMENA 123
MATHEMATICAL DESCRIPTIONS OF COMPLEX BINDING PHENOMENA 124
NON-LINEAR REGRESSION ANALYSIS OF COMPLEX BINDING PHENOMENA 131
INDEPENDENT RECEPTOR SUBTYPES 139
AFFINITY STATES OF A SINGLE RECEPTOR POPULATION 143
SUMMARY 152
5. THE PREPARATION AND STUDY OF DETERGENT-SOLUBILIZED RECEPTORS 157
GENERAL PROPERTIES OF BIOLOGICAL MEMBRANES AND DETERGENT MICELLES 158
CHOICE OF A BIOLOGICAL DETERGENT 167
SOLUBILIZING RECEPTORS FROM BIOLOGICAL MEMBRANES 169
METHODS FOR ANALYSIS OF DETERGENT-SOLUBILIZED RECEPTORS 171
SUMMARY 179
6. QUANTIFYING CELL SURFACE RECEPTOR BINDING AND TURNOVER IN INTACT CELLS 183
DISCRIMINATING BETWEEN CELL SURFACE VERSUS INTRACELLULAR RECEPTOR-LIGAND COMPLEXES 185
BIOCHEMICAL EVIDENCE CONSISTENT WITH RECYCLING OF CELL SURFACE RECEPTORS 191
ASSESSMENT OF RATE CONSTANTS FOR RECEPTOR TURNOVER USING A STEADY STATE MATHEMATICAL ANALYSIS OF INTACT CELL RADIOLIGAND BINDING DATA 195
THE HEAVY AMINO ACID DENSITY-SHIFT TECHNIQUE FOR QUANTITATING RECEPTOR SYNTHESIS AND TURNOVER 204
SUMMARY 206
INDEX 211