Receptor, Ligand and Transducer Contributions to Dopamine D2 Receptor Functional Selectivity.

ABSTRACT: Functional selectivity (or biased agonism) is a property exhibited by some G protein-coupled receptor (GPCR) ligands, which results in the modulation of a subset of a receptor's signaling capabilities and more precise control over complex biological processes. The dopamine D2 receptor (D2R) exhibits pleiotropic responses to the biogenic amine dopamine (DA) to mediate complex central nervous system functions through activation of G proteins and β-arrestins. D2R is a prominent therapeutic target for psychological and neurological disorders in which DA biology is dysregulated and targeting D2R with functionally selective drugs could provide a means by which pharmacotherapies could be developed. However, factors that determine GPCR functional selectivity in vivo may be multiple with receptors,

SUBMITTER: Peterson SM 

PROVIDER: S-EPMC4627803 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature