Recent findings leading to the discovery of selective dopamine D receptor ligands for the treatment of widespread diseases.

Since its discovery, the dopamine D receptor (DR) has been suggested to be an attractive target for the treatment of neuropsychiatric diseases. Novel findings have renewed the interest in such a receptor as an emerging target for the management of different diseases, including cancer, Parkinson's disease, alcohol or substance use disorders, eating disorders, erectile dysfunction and cognitive deficits. The recently resolved crystal structures of DR in complexes with the potent ligands nemonapride and L-745870 strongly improved the knowledge on the molecular mechanisms involving the DR functions and may help medicinal chemists in drug design. This review is focused on the recent development of the subtype selective DR ligands belonging to classical or new chemotypes. Moreover, ligands showing functional selectivity toward G protein activation or β-arrestin recruitment and the effects of selective DR ligands on the above-mentioned diseases are discussed.