Caccia S, Fong M H, Guiso G
Xenobiotica. 1985 Oct;15(10):835-44. doi: 10.3109/00498258509045035.
1-(2-Pyrimidinyl)-piperazine (PmP) is a common metabolite of the structurally related drugs buspirone, MJ-13805 and piribedil. After i.v. injection (25 mumol/kg) to rats, all three parent drugs are rapidly cleared with a t 1/2 (beta) of about 30 min. The metabolite t 1/2 is about four times that of its parent drugs. About 25, 23 and 2% of buspirone, MJ-13805 and piribedil, respectively, reaches the systemic circulation as PmP. The metabolite concentrates in the brain where its A.U.C. is about twice those of buspirone and MJ-13805. Results indicate that PmP formation is a pharmacologically significant process for both buspirone and MJ-13805 but it is probably less important for piribedil.
1-(2-嘧啶基)-哌嗪（PmP）是结构相关药物丁螺环酮、MJ-13805和吡贝地尔的常见代谢产物。给大鼠静脉注射（25 μmol/kg）后，所有三种母体药物均迅速清除，t 1/2（β）约为30分钟。代谢产物的t 1/2约为其母体药物的四倍。丁螺环酮、MJ-13805和吡贝地尔分别约有25%、23%和2%以PmP的形式进入体循环。该代谢产物在脑中浓缩，其AUC约为丁螺环酮和MJ-13805的两倍。结果表明，PmP的形成对丁螺环酮和MJ-13805而言是一个具有药理学意义的过程，但对吡贝地尔可能不太重要。
