Fused aminotetralins: Novel antagonists with high selectivity for the dopamine D3 receptor

Article abstract of DOI:10.1016/S0960-894X(98)00512-5

Starting from a series of 2-aminotetralins 1, a novel series of N-[4- (4-phenylbenzoylamino)butyl]-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine D₃ receptor has been designed. The effect of ligand chirality on binding affinity has been established. Selected derivatives (e.g. 2o, 2p) show high functional selectivity and enhanced in vivo properties compared to 1.