新型抗叶酸药物2,4-二氨基-5-金刚烷基-6-甲基嘧啶（DAMP）的研究：2,4-二氨基-5-金刚烷基-6-甲基嘧啶及其代谢产物的组织分布与处置
Studies with a new antifolate 2,4-diamino-5-adamantyl-6-methylpyrimidine (DAMP): tissue distribution and disposition of 2,4-diamino-5-adamantyl-6-methylpyrimidine and its metabolite.
作者信息
Zakrzewski S F, Dave C, Mead L H, Deluomo D S
出版信息
J Pharmacol Exp Ther. 1978 Apr;205(1):19-26.
The pharmacokinetics of a potentially useful antitumor agent, 2,4-diamino-5-adamantyl-6-methylpyrimidine (DAMP) has been studied in rat using 14C-labeled drug. It is reported that DAMP is metabolized rapidly by liver microsomes to an unidentified compound. The metabolite seems to be excreted by liver more rapidly than the unchanged drug, and within 24 hours all radioactivity is eliminated, 80% through kidney and 20% through the bile. Both DAMP, and its metabolite accumulate readily in pancreas and kidney. In contrast, in the brain mostly unchanged DAMP could be detected. The accumulation of the drug in tissues other than liver is much greater after i.v. than after i.p. administration.
使用14C标记的药物，在大鼠中研究了一种潜在有用的抗肿瘤药物2,4-二氨基-5-金刚烷基-6-甲基嘧啶（DAMP）的药代动力学。据报道，DAMP被肝微粒体迅速代谢为一种未鉴定的化合物。该代谢物似乎比未改变的药物更快地被肝脏排泄，并且在24小时内所有放射性都被消除，80%通过肾脏，20%通过胆汁。DAMP及其代谢物都很容易在胰腺和肾脏中蓄积。相比之下，在大脑中大多能检测到未改变的DAMP。静脉注射后，药物在肝脏以外组织中的蓄积比腹腔注射后要大得多。
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