The low affinity PCP sites in the rat cerebellum not only bind TCP-like but also BTCP-like structures

摘要: Congeners of the potent dopamine (DA) re-uptake inhibitor 1-[1-(2-benzo[b]thiophenyl)cyclohexyl]piperidine (BTCP) are unexpectedly able to bind in rat cerebellum, although this structure is devoid dopaminergic nerve endings. In line with previous studies hypothesis that they low affinity PCP sites labelled [3H]TCP even though do not high forebrain, was considered. Analogues 1-[1-(2-thiophenyl)cyclohexyl]piperidine (TCP) and BTCP a modified aromatic moiety O or S atoms substituted cyclohexyl ring were prepared tested competition experiments both forebrain cerebellum membranes [3H]TCP, striatum [3H]BTCP. Results indicated congeners could decrease selectivity for DA transporter. On contrary, some TCP analogues displayed very these sites; might be important pharmacological tools elucidate nature function at yet unknown sites.