Novel 6-substituted 2-aminotetralins with potent and selective affinity for the dopamine D3 receptor

Article abstract of DOI:10.1016/0960-894X(96)00043-1

Starting from (1S,2R)-5-methoxy-1-methyl-2-N,N-dipropylaminotetralin [(+)-UH-232] as a lead structure, a series of novel 6-substituted 2-aminotetralins have been discovered which show high affinity for dopamine D₃ receptors. One compound, GR218231, exhibits ca. 400 fold selectivity for the dopamine D₃ receptor over the D₂ receptor and ca. 10,000 fold selectivity with respect to D₁ and D₄ receptors.