1-(2-METHOXYPHENYL)-4-ALKYLPIPERAZINES: EFFECT OF THE N-4 SUBSTITUENT ON THE AFFINITY AND SELECTIVITY FOR DOPAMINE D4 RECEPTOR

Binding data on dopaminergic D2 and D4 and adrenergic α1 receptors of nine 1-(2-methoxyphenyl)piperazine derivatives are reported. The benzamide derivative 11 and ketone 12 displayed the highest affinity for human cloned D4 receptor (Ki = 1.3 nM and 1.7 nM, respectively). The former showed to be also selective versus D2 and α1 receptors. © 1997 Elsevier Science Ltd.