Recent Advances in the Development of Dopamine D3Receptor Antagonists: a Medicinal Chemistry Perspective

Abstract

Dopamine (DA) D₃ receptor antagonism might play a significant role in different therapeutic areas. A high number of preclinical studies on DA D₃ receptor antagonists have shown efficacy in animal models of Parkinson’s disease, schizophrenia and drug dependence. This Review covers the activities of medicinal chemists in this field over the last ten years towards the identification of truly selective compounds. Both primary and patent literature is reviewed here. Since the original discoveries, a clear trend towards the optimization of the developability properties of the new scaffold has clearly emerged with time, from both academic and industrial researchers. Examples of advanced leads from academia and industry are described. The latest potential therapeutic applications are reported too.