Desipramine and the phencyclidine derivative BTCP differently inhibit [3H]TCP binding to high- and low-affinity sites

The effects of N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine (BTCP) and desipramine on [3H]N-[1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP) binding were investigated in vivo and in vitro. In the cerebrum, both drugs were competitive inhibitors of high-affinity [3H]TCP binding. Conversely, in the cerebellum, they were non-competitive inhibitors of low-affinity [3H]TCP binding. These results imply that the different [3H]TCP binding sites have distinct pharmacological properties, and show that, although chemically related to TCP, BTCP has an effect similar to that of desipramine.