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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.

DOI:10.1016/0090-6980(88)90141-4
PMID:3399677
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。

相似文献

1
Mass spectrometric identification of urinary and plasma metabolites of 9-hydroxy-19,20-bis-nor-prostanoic acid (rosaprostol).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
Prostaglandins. 1988 May;35(5):665-84. doi: 10.1016/0090-6980(88)90141-4.
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Serum and urine kinetics of rosaprostol in volunteers.罗沙前列醇在志愿者体内的血清及尿液动力学
Arzneimittelforschung. 1988 Dec;38(12):1846-9.
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Prostaglandin cytoprotection in man: effectiveness of rosaprostol.人类前列腺素细胞保护作用:罗沙前列醇的有效性
Int J Tissue React. 1988;10(1):53-7.
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Mass spectrometric identification of urinary and plasma metabolites of 6-(6'-carboxyhexyl)-7-n-hexyl-1,3-diazaspiro-[4-4]-nonan-2,4-dione, a new cytoprotective agent.新型细胞保护剂6-(6'-羧基己基)-7-正己基-1,3-二氮杂螺[4.4]壬烷-2,4-二酮的尿液和血浆代谢物的质谱鉴定
Drug Metab Dispos. 1991 Sep-Oct;19(5):913-6.
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The effects of 9-hydroxy-19,20-bis-norprostanoic acid on mucus, acid and gastrin secretion in duodenal ulcer patients.9-羟基-19,20-双去甲前列腺酸对十二指肠溃疡患者黏液、胃酸及胃泌素分泌的影响
Prostaglandins Leukot Med. 1984 Aug;15(2):147-52. doi: 10.1016/0262-1746(84)90171-9.
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Platelet function, platelet prostanoids and vascular prostacyclin in diabetes mellitus.糖尿病中的血小板功能、血小板类前列腺素和血管前列环素
Prostaglandins Leukot Essent Fatty Acids. 1989 Mar;35(4):197-212. doi: 10.1016/0952-3278(89)90003-3.
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Nonprotein sulfhydryls as possible components of the protective effect of rosaprostol on the rat gastric mucosa.非蛋白质巯基作为罗沙前列醇对大鼠胃黏膜保护作用的可能组成成分。
Prostaglandins. 1985 Mar;29(3):467-74. doi: 10.1016/0090-6980(85)90104-2.
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Gastric antisecretory, antiulcer and cytoprotective properties of 9-hydroxy-19,20-bis-nor-prostanoic acid in experimental animals.9-羟基-19,20-双降前列腺酸在实验动物中的胃抗分泌、抗溃疡及细胞保护特性
Arzneimittelforschung. 1982;32(6):657-63.
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[Treatment of duodenal ulcer with rosaprostol in patients resistant to treatment with anti-H2].用罗沙前列醇治疗对抗H2治疗耐药的十二指肠溃疡患者
Minerva Med. 1987 Jun 30;78(12):847-53.
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[Further observations of the inhibitory effect of the disodium salt of 9-hydroxy-8,12-trans-19,20-bis-norprostanoic acid (rosaprostol) on gastric secretion].[9-羟基-8,12-反式-19,20-双降前列腺酸二钠盐(罗沙前列醇)对胃分泌抑制作用的进一步观察]
Farmaco Prat. 1984 Nov;39(11):409-16.

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Mass spectrometric identification of urinary and plasma metabolites of 2-(6'-carboxyhexyl)-3-n-hexylcyclohexylamine, a new antiaggregating agent.新型抗聚集剂2-(6'-羧基己基)-3-正己基环己胺的尿液和血浆代谢物的质谱鉴定
Eur J Drug Metab Pharmacokinet. 1992 Apr-Jun;17(2):93-101. doi: 10.1007/BF03188777.