A Molecular Basis for Selective Antagonist Destabilization of Dopamine D₃ Receptor Quaternary Organization.

ABSTRACT: The dopamine D₃ receptor (D₃R) is a molecular target for both first-generation and several recently-developed antipsychotic agents. Following stable expression of this mEGFP-tagged receptor, Spatial Intensity Distribution Analysis indicated that a substantial proportion of the receptor was present within dimeric/oligomeric complexes and that increased expression levels of the receptor favored a greater dimer to monomer ratio. Addition of the antipsychotics, spiperone or haloperidol, resulted in re-organization of D₃R quaternary structure to promote monomerization. This action was dependent on ligand concentration and reversed upon drug washout. By contrast, a number of other antagonists with high affinity at the D₃R, did not alter the dimer/monom

SUBMITTER: Marsango S 

PROVIDER: S-EPMC5437050 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature