Novel 6-substituted 2-aminotetralins with potent and selective affinity for the dopamine D3 receptor
作者:P.J. Murray、R.M. Helden、M.R. Johnson、G.M. Robertson、D.I.C. Scopes、M. Stokes、S. Wadman、J.W.F. Whitehead、A.G. Hayes、G.J. Kilpatrick、C. Large、C.M. Stubbs、M.P. Turpin
DOI:10.1016/0960-894x(96)00043-1
日期:1996.2
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 D-3 receptors. One compound, GR218231, exhibits ca. 400 fold selectivity for the dopamine D-3 receptor over the D-2 receptor and ca. 10,000 fold selectivity with respect to D-1 and D-4 receptors.