PCP receptor and dopamine uptake sites are discriminated by chiral TCP and BTCP derivatives of opposite configuration

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Summary 3-Methylpiperidine derivatives of 1-[1-(2-thienyl)cyclohexyl]piperidine (TCP) and l-[1-(2-benzo[ b ]thiophenyl)cyclohexyl] piperidine (BTCP) were obtained in their racemic and homochiral forms. They have been tested for their affinity for the PCP receptor labeled with [ 3 H]TCP and for the dopamine transporter labeled with [ 3 H]BTCP. The homochiral TCP derivative (+)- R displayed a very high affinity (5.2 nM) and selectivity for the PCP receptor. In contrast, the homochiral BTCP derivative (−)- S therefore of opposite configuration, displayed a very high affinity (3.5 nM) and selectivity for the dopamine transporter.