Caccia S, Conti I, Viganò G, Garattini S
Pharmacology. 1986;33(1):46-51. doi: 10.1159/000138199.
Buspirone (BP), a newly developed antianxiety agent, forms 1-(2-pyrimidinyl)-piperazine (PmP) during its biotransformation in rats and man. After oral administration of pharmacologically effective doses of BP-hydrochloride to rats (1 and 10 mg/kg), the metabolite appears in significant amounts in body fluids and tissues; it is highly concentrated in the central nervous system, the brain-to-plasma concentration ratios being approximately 5 at the time of the maximum concentrations (Cmax). In man given the anxiolytic dose (20 mg) of BP the metabolite reaches higher plasma Cmax values than its parent drug. Its plasma elimination t1/2 is more than double that for BP. These results, together with the fact that PmP is biochemically and pharmacologically active, suggest that the metabolite may contribute significantly to the central effects of the parent drug.
丁螺环酮（BP）是一种新开发的抗焦虑药物，在大鼠和人体内进行生物转化时会形成1-（2-嘧啶基）-哌嗪（PmP）。给大鼠口服药理有效剂量的盐酸丁螺环酮（1和10mg/kg）后，该代谢产物在体液和组织中大量出现；它在中枢神经系统中高度浓缩，在最大浓度（Cmax）时脑与血浆的浓度比约为5。在给予抗焦虑剂量（20mg）丁螺环酮的人体中，该代谢产物的血浆Cmax值高于其母体药物。其血浆消除半衰期比丁螺环酮长一倍多。这些结果，再加上PmP具有生化和药理活性这一事实，表明该代谢产物可能对母体药物的中枢作用有显著贡献。
