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9-羟基-19,20-双去甲前列腺酸(罗沙前列醇)尿液和血浆代谢物的质谱鉴定

Mass spectrometric identification of urinary and plasma metabolites of 9-hydroxy-19,20-bis-nor-prostanoic acid (rosaprostol).

作者信息

Benfenati E, Fanelli R, Chiabrando C, Valcavi U, Bosone E, Farina P

机构信息

Laboratory of Environmental Pharmacology and Toxicology, Istituto di Ricerche Farmacologiche Mario Negri, Milan, Italy.

出版信息

Prostaglandins. 1988 May;35(5):665-84. doi: 10.1016/0090-6980(88)90141-4.

Abstract

9-Hydroxy-19,20-bis-nor-prostanoic acid (Rosaprostol) is an antiulcer compound with antisecretory and cytoprotective action. We studied the metabolites of Rosaprostol found in human plasma and in human and rat urine. Sixteen different metabolites were tentatively identified on the basis of their mass spectra. Two presumed metabolites were synthesized. To clarify the identities of some of them, deuterated Rosaprostol was administered to rats and mass spectra of the deuterated and protonated metabolites were examined. Rosaprostol is metabolized following three metabolic pathways leading, combined, to oxidized compounds with a lower number of carbons than the parent drug.

摘要

9-羟基-19,20-双降前列腺酸(罗沙前列醇)是一种具有抗分泌和细胞保护作用的抗溃疡化合物。我们研究了罗沙前列醇在人血浆、人尿和大鼠尿中的代谢产物。根据其质谱初步鉴定出16种不同的代谢产物。合成了两种推测的代谢产物。为了明确其中一些代谢产物的身份,给大鼠施用氘代罗沙前列醇,并检测氘代和质子化代谢产物的质谱。罗沙前列醇通过三种代谢途径进行代谢,综合起来会产生比母体药物碳原子数更少的氧化化合物。

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