Cell Surface Receptors: A Short Course on Theory and Methods, Second Edition is a primer for the study of cell surface receptors. The simplified discussion of methods and their underlying principles removes the usual intimidation caused by the specialized vocabulary or sophisticated mathematics that characterize many of the primary papers in this field. In this way, the basic concepts become emphasized. This volume is a starting point: a textbook as well as a manual to which the investigator can return for a refresher course, when needed.
Cell Surface Receptors: A Short Course on Theory and Methods, SecondEdition is a primer for the study of cell surface receptors. The simplified discussion of methods and their underlying principles removes the usual intimidation caused by the specialized vocabulary or sophisticated mathematics that characterize many of the primary papers in this field. In this way, the basic concepts become emphasized. This volume is a starting point: a textbook as well as a manual to which the investigator can return for a refresher course, when needed.Hinweis: Dieser Artikel kann nur an eine deutsche Lieferadresse ausgeliefert werden.
1 Historical perspective.- The origin of the receptor concept.- Mass action law and occupancy theory.- The concept of efficacy.- The concept of spare receptors.- Rate theory.- Allosteric theory.- Operational models of pharmacological agonism.- Summary.- 2 Methods for characterization of receptors based on receptor-mediated responses in tissue or intact cell preparations.- Characterization of receptor specificity.- Generalizations regarding the determination of equilibrium dissociation constants (KD values) for receptor-ligand interactions in intact tissue preparations.- Determination of KD values for receptor-agonist interactions, KDA.- Determination of KD values for receptor-partial agonist interactions, KDP.- Determination of KD values for receptor-antagonist interactions, KDB.- Summary.- 3 Identification of receptors using direct radioligand binding techniques.- Methods-data generation.- Choice of a radioligand.- The incubation.- Separation of bound from free radioligand.- Criteria expected for binding of D to the physiological receptor, R.- Data obtained to establish the criteria for a physiologically relevant receptor.- Summary.- 4 Complex binding phenomena.- Mathematical descriptions of complex binding phenomena.- Computer-assisted analysis of complex binding phenomena.- Analysis of receptor subtypes.- Independent data consistent with the existence of receptor subtypes.- Receptor affinity states.- The ternary complex model (TCM) and expansions of the TCM.- Thermodynamic parameters of receptor-ligand interactions.- Summary.- 5 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 ofdetergent-solubilized receptors.- Summary.- 6 The topographical fate of ligand-receptor complexes as reflected by the properties of ligand binding to intact cells.- Biochemical approaches for discriminating between cell surface receptors 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.
1 Historical perspective.- The origin of the receptor concept.- Mass action law and occupancy theory.- The concept of efficacy.- The concept of spare receptors.- Rate theory.- Allosteric theory.- Operational models of pharmacological agonism.- Summary.- 2 Methods for characterization of receptors based on receptor-mediated responses in tissue or intact cell preparations.- Characterization of receptor specificity.- Generalizations regarding the determination of equilibrium dissociation constants (KD values) for receptor-ligand interactions in intact tissue preparations.- Determination of KD values for receptor-agonist interactions, KDA.- Determination of KD values for receptor-partial agonist interactions, KDP.- Determination of KD values for receptor-antagonist interactions, KDB.- Summary.- 3 Identification of receptors using direct radioligand binding techniques.- Methods-data generation.- Choice of a radioligand.- The incubation.- Separation of bound from free radioligand.- Criteria expected for binding of D to the physiological receptor, R.- Data obtained to establish the criteria for a physiologically relevant receptor.- Summary.- 4 Complex binding phenomena.- Mathematical descriptions of complex binding phenomena.- Computer-assisted analysis of complex binding phenomena.- Analysis of receptor subtypes.- Independent data consistent with the existence of receptor subtypes.- Receptor affinity states.- The ternary complex model (TCM) and expansions of the TCM.- Thermodynamic parameters of receptor-ligand interactions.- Summary.- 5 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 ofdetergent-solubilized receptors.- Summary.- 6 The topographical fate of ligand-receptor complexes as reflected by the properties of ligand binding to intact cells.- Biochemical approaches for discriminating between cell surface receptors 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.
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