Novel 6-Substituted 2-Aminotetralins with Potent and Selective Affinity for the Dopamine D3 Receptor.

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.