Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.

Table of Contents:
Theoretical and Mechanistic Aspects of Functional Selectivity.- Historical Overview of the Concept of Functional Selectivity.- Functional Selectivity: Theoretical Considerations and Future Directions.- Agonist-Selective Coupling of G Protein-Coupled Receptors.- Ligand-Selective Receptor Desensitization and Endocytosis.- Selectivity for G Protein or Arrestin-Mediated Signaling.- In Vivo Evidence for and Consequences of Functional Selectivity.- Subfamilies of Therapeutically Relevant Receptors.- Functional Selectivity at Adrenergic Receptors.- Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity.- Functional Selectivity at Serotonin Receptors.- Functional Selectivity at Dopamine Receptors.- Functional Selectivity at Receptors for Cannabinoids and Other Lipids.- Functional Selectivity at Opioid Receptors.- Functional Selectivity at Non-Opioid Peptide Receptors.