4-羟基咪达唑仑
4-羟基咪达唑仑结构式
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常用名 | 4-羟基咪达唑仑 | 英文名 | 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-4-ol |
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| CAS号 | 59468-85-8 | 分子量 | 341.76700 | |
| 密度 | 1.44g/cm3 | 沸点 | 550.6ºC at 760 mmHg | |
| 分子式 | C18H13ClFN3O | 熔点 | 186-187ºC | |
| MSDS | 美版 | 闪点 | 286.8ºC |
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A comparison of the metabolism of midazolam in C57BL/6J and hepatic reductase null (HRN) mice.
Biochem. Pharmacol. 92(4) , 701-11, (2014) The hepatic cytochrome P450 reductase null (HRN) mouse, which has no functional hepatic Cyp P450s, may represent a useful model for examining extra-hepatic P450-related oxidative metabolism. Here the pharmacokinetics and metabolic fate of midazolam, a drug kn... |
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Systematic evaluation of commercially available ultra-high performance liquid chromatography columns for drug metabolite profiling: optimization of chromatographic peak capacity.
J. Chromatogr. A. 1374 , 122-33, (2014) The present study investigated the practical use of modern ultra-high performance liquid chromatography (UHPLC) separation techniques for drug metabolite profiling, aiming to develop a widely applicable, high-throughput, easy-to-use chromatographic method, wi... |
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Species differences and substrate specificity of CYP3A heteroactivation by efavirenz.
Xenobiotica 45(4) , 345-52, (2015) 1. The purpose of this study was to clarify species differences in the heteroactivation of CYP3A substrates by efavirenz, which is known from clinical studies to activate midazolam 1'-hydroxylation, and to assess the feasibility of an animal model. 2. In monk... |
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Development of Murine Cyp3a Knockout Chimeric Mice with Humanized Liver.
Drug Metab. Dispos. 43 , 1208-17, (2015) We developed murine CYP3A knockout ko chimeric mice with humanized liver expressing human P450S similar to those in humans and whose livers and small intestines do not express murine CYP3A this: approach may overcome effects of residual mouse metabolic enzyme... |
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A highly sensitive liquid chromatography tandem mass spectrometry method for simultaneous quantification of midazolam, 1'-hydroxymidazolam and 4-hydroxymidazolam in human plasma.
Biomed. Chromatogr. 25(10) , 1091-8, (2011) A highly sensitive liquid chromatography-tandem mass spectrometry method for the simultaneous quantification of midazolam and its major metabolites 1'-hydroxymidazolam and 4-hydroxymidazolam in human plasma was developed and validated. Stable isotope-labeled ... |
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Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cdna-expressed human cytochrome P450.
Drug Metab. Dispos. 24(9) , 940-7, (1996) Midazolam (MDZ) is metabolized in human liver microsomes by the cytochrome P450 (CYP) 3A subfamily to 1'-hydroxy (1'-OH) and 4-hydroxy (4-OH) metabolites. MDZ is metabolized in the rat primarily to 4-OH MDZ, 1'-OH MDZ, and 1',4-dihydroxy (1',4-diOH) MDZ. The ... |
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Evidence of CYP3A allosterism in vivo: analysis of interaction between fluconazole and midazolam.
Clin. Pharmacol. Ther. 91(3) , 442-9, (2012) The allosteric effect of fluconazole (effector) on the formation of 1'-hydroxymidazolam (1'-OH-MDZ) and 4-hydroxymidazolam (4-OH-MDZ) from midazolam (MDZ), a substrate of CYP3A4/5--members of the cytochrome P450 superfamily of enzymes--was examined in healthy... |
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Simultaneous determination of midazolam and its metabolites 1-hydroxymidazolam and 4-hydroxymidazolam in human serum using gas chromatography-mass spectrometry.
J. Chromatogr. B. Biomed. Sci. Appl. 692(1) , 95-100, (1997) A method for the quantitation of midazolam and its metabolites 1-hydroxymidazolam and 4-hydroxymidazolam from human serum capable of monitoring concentrations achieved under therapeutic conditions is presented. The substances were extracted under basic condit... |
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Expression of the human CYP3A4 gene in the small intestine of transgenic mice: in vitro metabolism and pharmacokinetics of midazolam.
Drug Metab. Dispos. 31(5) , 548-58, (2003) Human cytochrome P450 3A4 (CYP3A4) is the most abundant hepatic and intestinal phase I drug-metabolizing enzyme, and participates in the oxidative metabolism of approximately 50% of drugs on the market. In the present study, a transgenic-CYP3A4 (Tg-CYP3A4) mo... |
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Ultrafast liquid chromatography/tandem mass spectrometry bioanalysis of polar analytes using packed silica columns.
Rapid Commun. Mass Spectrom. 16(17) , 1613-21, (2002) Ultrafast liquid chromatography/tandem mass spectrometry (LC/MS/MS) bioanalysis was demonstrated with the use of packed silica columns operated under elevated flow rates. A special effort has been made to achieve ultrafast analysis without sacrificing chromat... |