Cell Surface Receptors: A Short Course on Theory and Methods

Introduction to Receptor Theory - Origin of the Receptor Concept - Occupancy Theory -Relationship Between Occupancy and Response - Concept of Spare Receptors - Operational Models of Pharmacological Agonism - Rate Theory - Allosteric Theory - Beyond Two-State Receptor Theory - Summary.- Characterization of Receptors Based on Receptor-Mediated Responses - Characterization of Receptor Specificity - Determining Equilibrium Dissociation Constants (Kd Values) for Receptor-Ligand Interactions Based on Measurements of Receptor-Mediated Response - Pharmacologic Resultant Analysis - Summary.- Identification of Receptors Using Direct Radioligand Binding Techniques - Methods - Data Generation - Criteria Expected for Binding of *D to the Physiologically Relevant Receptor, R - Determination of Rate Constants for Radioligand Association and Dissociation - Summary.- Complex Binding Phenomena - Mathematical Descriptions of Complex Binding Phenomena 124 - Non-Linear Regression Analysis of Complex Binding Phenomena - Independent Receptor Subtypes - Affinity States of a Single Receptor Population - Summary.- The Preparation and Study of Detergent-Solubilized Receptors - General Properties of Biological Membranes and Detergent Micelles - Choice of a Biological Detergent - Solubilizing Receptors from Biological Membranes - Methods for Analysis of Detergent-Solubilized Receptors - Summary.- Quantifying Cell Surface Receptor Binding and Turnover in Intact Cells - Discriminating Between Cell Surface Versus Intracellular Receptor-Ligand Complexes - Biochemical Evidence Consistent with Recycling of Cell Surface Receptors - Assessment of Rate Constants for Receptor Turnover Using a Steady State Mathematical Analysis of Intact Cell Radioligand Binding Data - The Heavy Amino Acid Density-Shift Technique for Quantitating Receptor Synthesis and Turnover - Summary.- Index.