Diverse arrestin-recruiting and endocytic profiles of tricyclic antipsychotics acting as direct α_2A adrenergic receptor ligands.

ABSTRACT: The therapeutic mechanism of action underlying many psychopharmacological agents remains poorly understood, due largely to the extreme molecular promiscuity exhibited by these agents with respect to potential central nervous system targets. Agents of the tricyclic chemical class, including both antidepressants and antipsychotics, exhibit a particularly high degree of molecular promiscuity; therefore, any clarification of how these agents interact with specific central nervous system targets is of great potential significance to the field. Here, we present evidence demonstrating that tricyclic antipsychotics appear to segregate into three distinct groups based upon their molecular interactions with the centrally-important α_2A adrenergic receptor (AR). Specifically, while the α

SUBMITTER: Cottingham C 

PROVIDER: S-EPMC5385157 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature