鎮痛剤に関する研究(第14報)1-n-Butyryl-4-cinnamyl[γ-^<14>C]piperazine Hydrochloride(BCP-^<14>C)のラットにおける吸収, 排泄, 体内分布および代謝について

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In order to study the metabolic fate of 1-butyryl-4-cinnamylpiperazine hydrochloride (BCP), a new analgesic drug, 1-butyryl-4-cinnamyl [γ-^<14>C] piperazine hydrochloride (BCP-^<14>C) was administered subcutaneously to the rat at a dose of 20 mg/kg. The highest concentration of ^<14>C-activity in blood was found 20 min after administration of BCP-^<14>C. About 27% and 49% of the administered ^<14>C-activity were excreted in the 24 hr urine and feces, respectively. The distribution of BCP-^<14>C in the rat was detected by the wholebody autoradiogram and the ^<14>C-activity of each tissue was determined by a liquid scintillation counter. Major metabolites in the urine were BCP, 1-butyryl-4-(4'-hydroxy) cinnamylpiperazine (p-OH-BCP), 4-hydroxycinnamylpiperazine (p-OH-CP), benzoic acid, and hippuric acid. On the other hand, p-OH-BCP, p-OH-CP, and their conjugates were the major metabolites in the bile. These results suggested that the major metabolic pathway of BCP in the rat was the para-hydroxylation. The ^<14>C-activity in the liver (66.6%) was identified as BCP, p-OH-BCP, cinnamylpiperazine, p-OH-CP, and cinnamic acid. In the brain, 0.84% of the administered ^<14>C-activity was found at 20 min after the administation and almost all of the ^<14>C-activity (94.5%) originated from unchanged BCP.
社団法人日本薬学会の論文
1974-07-25