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.
INSERM U 336, Ecole Nationale Supérieure de Chimie, Montpellier, France.
T
T
Maurice
J
J
Vignon
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001933:Brain Stem / Q000187:drug effects / Q000378:metabolism; D002531:Cerebellum / Q000187:drug effects / Q000378:metabolism; D003891:Desipramine / Q000494:pharmacology*; D015259:Dopamine Agents / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051379:Mice; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats
D015259:Dopamine Agents; C056415:1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine; C012058:tenocyclidine; D010622:Phencyclidine; D003891:Desipramine