The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems - Hardcover

by Terry P. Kenakin (Author), James A. Angus (Author), T. Kenakin (Author)

1. Introduction: Bioassays--Past Uses and Future Potential. Section I: Classical Pharmacology and Isolated Tissue Systems. 1.Human Vascular Receptors in Disease: Pharmacodynamic Analyses in Isolated Tissue. 2. Problems in Assigning Mechanisms: Reconciling the Molecular and Functional Pathways in Alpha-Adrenoceptor-Mediated Vasoconstriction. 3. Gs Protein-Coupled Receptors in Human Heart. Section II: New Theoretical Concepts and Molecular Mechanisms of Receptor Function. 4. Kinetic Modeling Approaches to Understanding Ligand Efficacy. 5. The Evolution of Drug-Receptor Models: The Cubic Ternary-Complex Model for G Protein-Coupled Receptors. 6. Inverse Agonism. 7. Efficacy: Molecular Mechanisms and Operational Methods of Measurement. A New Algorithm for the Prediction of Side Effects. 8. A Look at Receptor Efficacy. From the Signalling Network of the Cell to the Intramolecular Motion of the Receptor. 9. Mechanisms of Non-Competitive Antagonism and Co-Agonism. 10. Mechanisms of Receptor Activation and the Relationship to Receptor Structure. Section III: New Technologies for the Study of Drug Receptor Interaction. 11. The Assembly of Recombinant Receptor Systems and Their Use to Investigate Signalling Dynamics. 12. Insect Cell Systems to Study the Communication of Mammalian Receptors and G Proteins. 13. Altering the Relative Stoichiometry of Receptors, G Proteins and Effectors: Effects on Agonist Function. 14. The Study of Drug-Receptor Interaction Using Reporter Gene Systems in Mammalian Cells. 15. Melanophore Recombinant Receptors Systems.