Functional Selectivity of G Protein-Coupled Receptor Ligands New Opportunities for Drug Discovery /

• Corporate Author: SpringerLink (Online service)
• Other Authors: Neve, Kim A. (Editor)
• Format: Electronic eBook
• Language: English
• Published: Totowa, NJ : Humana Press, 2009.
• Series: The Receptors
• Subjects: Medicine.; Human physiology.; Neurosciences.; Pharmacology.; Neurology.; Neurobiology.; Biomedicine.; Pharmacology/Toxicology.; Human Physiology.

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 p...

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.