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Stereoselective binding of 3-acetoxy-, and 3-hydroxy-1,4-benzodiazepine-2-ones to human serum albumin. Selective allosteric interaction with warfarin enantiomers.

作者信息

Fitos I, Tegyey Z, Simonyi M, Sjöholm I, Larsson T, Lagercrantz C

出版信息

Biochem Pharmacol. 1986 Jan 15;35(2):263-9. doi: 10.1016/0006-2952(86)90524-1.

DOI:10.1016/0006-2952(86)90524-1
PMID:3942599
Abstract

Stereoselective binding of oxazepam, lorazepam, temazepam and methyl lorazepam as well as of their acetates to human serum albumin was investigated by different techniques. The 2'-chlorine and the N(1)-methyl substitution exert opposite effects on the antipodes. Enantiomers of oxazepam acetate (OAc) and lorazepam acetate (LAc) displace diazepam. Allosteric interactions with warfarin were manifested by either mutually increased or decreased binding depending on the structure of benzodiazepine and on the configuration of both benzodiazepine and warfarin. The most remarkable effect could be observed in the simultaneous binding of (S)-lorazepam acetate and (S)-warfarin.

摘要

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引用本文的文献

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Demonstration of stereoselective disposition of warfarin enantiomers by whole-body autoradiography.通过全身放射自显影术证明华法林对映体的立体选择性分布。
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2
Chirality. Clinical pharmacokinetic and pharmacodynamic considerations.手性。临床药代动力学和药效学考量。
Clin Pharmacokinet. 1990 May;18(5):339-45. doi: 10.2165/00003088-199018050-00001.