Functional Selectivity, Ligand-Directed Trafficking, Conformation-Specific Agonism: What’s In A Name?

Terms that may fall under the umbrella of functional selectivity. The ability of a ligand to place a receptor in multiple conformations that lead to different intracellular signal transduction events has been described by a number of terms as indicated under the umbrella above. The variety of the terms illustrates the richness of the pharmacology that has been revealed in this area. A standardized nomenclature has yet to be defined. Figure inspired by Arthur Christopoulos.