A novel series of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor

Article abstract of DOI:10.1016/S0960-894X(97)00350-8

A novel series of N-[4-(4-Phenylbenzoylamino)butyl]-1,2,3,4-tetrahydro-2-naphthylamines with high affinity and selectivity for the dopamine D₃ receptor has been prepared. The 5-cyclopropylmethyloxy 3j, methanesulfonyloxy 3k and trifluoromethanesulfonyloxy 3l derivatives represent some of the highest affinity (pKi's 8.6-8.9) and most selective (200-320-fold) dopamine D₃ receptor antagonists reported to date.