AN EVOLUTIONARY VIEW OF DRUG-RECEPTOR INTERACTION - THE BIOAMINE RECEPTOR FAMILY

The large molecular diversity of receptors and their subtypes means th at the pharmacologist is faced with many puzzling characterization que stions. First, the molecular diversity of the receptors is deciphered only in part by a pharmacological approach, which precludes a satisfac tory receptor classification based solely on pharmacological character istics. Second, the physiological counterpart of the numerous subtypes of receptors specifically activated by single endogenous ligands rema ins unclear. Here, Philippe Vernier and colleagues use the example of the bioamine G protein-coupled receptors to show that many of the appa rent inconsistencies that emerge from pharmacological and molecular ch aracterizations of receptors can be better understood if the evolution ary history of the receptors is taken into account.