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Comparison of dihydrodiazepam enantiomers: metabolism, serum binding and brain receptor binding.

作者信息

Tegyey Z, Maksay G, Kardos J, Otvös L

出版信息

Experientia. 1980 Sep 15;36(9):1031-2. doi: 10.1007/BF01965950.

DOI:10.1007/BF01965950
PMID:7418834
Abstract

Dihydrodiazepam is a diazepam prodrug, as shown by its in vitro metabolism by rat and mouse liver and brain microsomal fractions, and its displacing activity on brain diazepam binding. The mechanism of bioactivation is discussed. Stereoselectivity of metabolism and of binding to specific benzodiazepine binding sites in brain synpatosomes and serum albumin were studied.

摘要

相似文献

1
Comparison of dihydrodiazepam enantiomers: metabolism, serum binding and brain receptor binding.
Experientia. 1980 Sep 15;36(9):1031-2. doi: 10.1007/BF01965950.
2
Metabolism of levorotary 4,5-dihydrodiazepam in the rat.左旋4,5-二氢地西泮在大鼠体内的代谢
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Diazepam receptor characterization: specific binding of a benzodiazepine to macromolecules in various areas of rat brain.地西泮受体特性：一种苯二氮䓬与大鼠脑不同区域大分子的特异性结合。
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Benzodiazepine receptor: demonstration in the central nervous system.苯二氮䓬受体：在中枢神经系统中的显示
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引用本文的文献

1
Stereoselective binding of 4,5-dihydrodiazepam to human serum albumin.4,5-二氢地西泮与人血清白蛋白的立体选择性结合。
Experientia. 1983 Jun 15;39(6):591-2. doi: 10.1007/BF01971111.

本文引用的文献

1
Analytical and pharmacokinetic studies on the optic isomers of oxazepam succinate half-ester.琥珀酸奥沙西泮半酯光学异构体的分析及药代动力学研究。
Biochem Pharmacol. 1972 Jan;21(1):127-9. doi: 10.1016/0006-2952(72)90260-2.
2
Microsomal oxidase. IV. Properties of a mixed-function amine oxidase isolated from pig liver microsomes.微粒体氧化酶。IV. 从猪肝微粒体中分离出的一种混合功能胺氧化酶的性质。
Arch Biochem Biophys. 1972 May;150(1):116-25. doi: 10.1016/0003-9861(72)90017-3.
3
[Pharmacological study of the optically active modifications of 1,3,4,5-tetrahydro-1,4-benzodiazepine-2-one].
[1,3,4,5-四氢-1,4-苯并二氮杂䓬-2-酮光学活性变体的药理学研究]
Acta Pharm Hung. 1973 Sep;43(5):218-23.
4
Stereostructure-activity relationships for oxazepam hemisuccinate. Effects on central nervous system.
Arzneimittelforschung. 1972 Aug;22(8):1328-33.
5
Metabolism and anticonvulsant activity of deuterated N-demethyldiazepam.氘代N-去甲基地西泮的代谢与抗惊厥活性
J Pharm Sci. 1973 Nov;62(11):1900-2. doi: 10.1002/jps.2600621144.
6
Examination of the metabolism in vitro of parathion (diethyl p-nitrophenyl phosphorothionate) by rat lung and brain.大鼠肺和脑对对硫磷（二乙基对硝基苯基硫代磷酸酯）的体外代谢研究。
Biochem Pharmacol. 1976 Jan;25(1):37-45. doi: 10.1016/0006-2952(76)90170-2.
7
Benzodiazepine receptor: demonstration in the central nervous system.苯二氮䓬受体：在中枢神经系统中的显示
Science. 1977 Nov 25;198(4319):849-51. doi: 10.1126/science.918669.
8
Benzodiazepine receptors in rat brain.大鼠脑中的苯二氮䓬受体。
Nature. 1977 Apr 21;266(5604):732-4. doi: 10.1038/266732a0.
9
Stereospecificity of esterases hydrolyzing oxazepam acetate.水解奥沙西泮乙酸酯的酯酶的立体特异性
J Pharm Sci. 1978 Sep;67(9):1208-10. doi: 10.1002/jps.2600670905.
10
Stereospecific benzodiazepine receptor binding by the enantiomers of oxazepam sodium hemisuccinate.奥沙西泮半琥珀酸钠对映体的立体特异性苯二氮䓬受体结合作用
Neuropharmacology. 1978 Mar;17(3):215-6. doi: 10.1016/0028-3908(78)90103-x.