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顺铂衍生物 -3H-顺式-1,2-二氨基环己烷二氯铂(II)和 3H-顺式-1,2-二氨基环己烷丙二酸铂(II)在 BDF1 小鼠体内的处置情况。

Disposition of cisplatin derivatives -3H-cis-1,2-diaminocyclohexanedichloroplatinum (II) and 3H-cis-1,2-diaminocyclohexanemalonatoplatinum (II) in BDF1 mice.

作者信息

Oswald C B, Wyrick S D, Chaney S G, Shrewsbury R O, Hall I H

机构信息

Division of Medicinal Chemistry, School of Pharmacy, University of North Carolina, Chapel Hill 27599.

出版信息

Res Commun Chem Pathol Pharmacol. 1989 Apr;64(1):41-58.

PMID:2749002
Abstract

The disposition of 3H-cis-1,2-diaminocyclohexanedichloroplatinum (II) and 3H-cis-1,2-diaminocyclohexanemalonatoplatinum (II) was investigated in P388 tumor-bearing BDF1 mice. Fifteen minutes after IP administration of the drugs, the serum contained 12% of the 3H-chloride derivative and 20% of the malonate derivative. Both drugs distributed to all organs of the body but were not sequestered in any major internal organ. However, substantial amounts of the drugs were found in the carcass and skin. After 24 hr, approximately 43% of the radioactivity was excreted in the urine. Only 5 to 8% of the radioactivity was eliminated in the feces. The radioactivity half-life (t1/2 beta) for the 3H-chloride derivative was estimated from urinary excretion data to be 22.7 hr, and 30.0 hr for the 3H-malonate derivative.

摘要

在携带P388肿瘤的BDF1小鼠中研究了3H-顺式-1,2-二氨基环己烷二氯铂(II)和3H-顺式-1,2-二氨基环己烷丙二酸铂(II)的处置情况。腹腔注射药物15分钟后,血清中含有12%的3H-氯化物衍生物和20%的丙二酸酯衍生物。两种药物均分布于身体的所有器官,但未在任何主要内部器官中蓄积。然而,在尸体和皮肤中发现了大量的药物。24小时后,约43%的放射性从尿液中排出。只有5%至8%的放射性从粪便中消除。根据尿液排泄数据估计,3H-氯化物衍生物的放射性半衰期(t1/2β)为22.7小时,3H-丙二酸酯衍生物为30.0小时。

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