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马来酸氟伏沙明:人体代谢

Fluvoxamine maleate: metabolism in man.

作者信息

Overmars H, Scherpenisse P M, Post L C

出版信息

Eur J Drug Metab Pharmacokinet. 1983 Jul-Sep;8(3):269-80. doi: 10.1007/BF03188757.

DOI:10.1007/BF03188757
PMID:6418548
Abstract

The metabolic fate of fluvoxamine maleate in man was investigated. The metabolites were isolated from the pooled urines of healthy volunteers who had ingested either 5 mg radioactive, or 100 mg non-radioactive fluvoxamine maleate as a single dose. The main isolation methods were solvent extraction, column and thin-layer chromatography. Eleven metabolites were isolated; eight of these were carboxylic acids. Identification of nine metabolites was accomplished by mass spectrometry supported by information from the UV spectra and the ionogenic properties. The main route of metabolic degradation of fluvoxamine begins with oxidative elimination of the methoxyl group, another route with removal of the primary amino group. In view of the nature of the degradation pattern none of the metabolites is likely to possess psychotropic activity. For the two primary metabolites this has, in effect, been demonstrated.

摘要

对马来酸氟伏沙明在人体内的代谢命运进行了研究。代谢物是从健康志愿者的混合尿液中分离出来的,这些志愿者单次服用了5毫克放射性或100毫克非放射性马来酸氟伏沙明。主要的分离方法是溶剂萃取、柱色谱和薄层色谱。分离出了11种代谢物;其中8种是羧酸。通过质谱并结合紫外光谱和离子性质信息完成了9种代谢物的鉴定。氟伏沙明的主要代谢降解途径始于甲氧基的氧化消除,另一条途径是伯氨基的去除。鉴于降解模式的性质,没有一种代谢物可能具有精神活性。对于两种主要代谢物,实际上已经证明了这一点。

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Development of a Physiologically Based Pharmacokinetic/Pharmacodynamic Model to Predict the Impact of Genetic Polymorphisms on the Pharmacokinetics and Pharmacodynamics Represented by Receptor/Transporter Occupancy of Central Nervous System Drugs.
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In silico and intuitive predictions of CYP46A1 inhibition by marketed drugs with subsequent enzyme crystallization in complex with fluvoxamine.计算机预测和直观预测显示,上市药物可抑制 CYP46A1,随后用氟伏沙明与酶共结晶。
Mol Pharmacol. 2012 Nov;82(5):824-34. doi: 10.1124/mol.112.080424. Epub 2012 Aug 2.
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Fluvoxamine in the treatment of anxiety disorders.氟伏沙明治疗焦虑障碍。
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Cell Mol Neurobiol. 1999 Aug;19(4):467-89. doi: 10.1023/a:1006986824213.