PCP RECEPTOR AND DOPAMINE UPTAKE SITES ARE DISCRIMINATED BY CHIRAL TCP AND BTCP DERIVATIVES OF OPPOSITE CONFIGURATION

3-Methylpiperidine derivatives of 1-[1-(2-thienyl)cyclohexyl]piperidin e (TCP) and 1-[1-(2-benzo[b]thiophenyl)cyclohexyl]piperidine (BTCP) we re obtained in their racemic and homochiral forms. They have been test ed for their affinity for the PCP receptor labeled with [H-3]TCP and f or the dopamine transporter labeled with [H-3]BTCP. The homochiral TCP derivative (+)-R displayed a very high affinity (5.2 nM) and selectiv ity for the PCP receptor. In contrast, the homochiral BTCP derivative (-)-S, therefore of opposite configuration, displayed a very high affi nity (3.5 nM) and selectivity for the dopamine transporter.