1-羟基咪达唑仑结构式
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常用名 | 1-羟基咪达唑仑 | 英文名 | 1'-Hydroxymidazolam |
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| CAS号 | 59468-90-5 | 分子量 | 341.767 | |
| 密度 | 1.4±0.1 g/cm3 | 沸点 | 540.6±60.0 °C at 760 mmHg | |
| 分子式 | C18H13ClFN3O | 熔点 | 264-266ºC | |
| MSDS | 美版 | 闪点 | 280.7±32.9 °C | |
| 符号 |
GHS02, GHS06, GHS08 |
信号词 | Danger |
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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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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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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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Metabolism of 1'- and 4-hydroxymidazolam by glucuronide conjugation is largely mediated by UDP-glucuronosyltransferases 1A4, 2B4, and 2B7.
Drug Metab. Dispos. 38(11) , 2007-13, (2010) Midazolam undergoes oxidative hydroxylation by CYP3A to its metabolites, which are excreted mainly as glucuronidated conjugates into the urine. In this study, we examined the glucuronidation of hydroxymidazolam in human liver microsomes (HLMs) and characteriz... |
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The structural basis for homotropic and heterotropic cooperativity of midazolam metabolism by human cytochrome P450 3A4.
Biochemistry 50(50) , 10804-18, (2011) Human cytochrome P450 3A4 (CYP3A4) metabolizes a significant portion of clinically relevant drugs and often exhibits complex steady-state kinetics that can involve homotropic and heterotropic cooperativity between bound ligands. In previous studies, the hydro... |
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Development and validation of a rapid and sensitive assay for simultaneous quantification of midazolam, 1′-hydroxymidazolam, and 4-hydroxymidazolam by liquid chromatography coupled to tandem mass-spectrometry
J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 878(19) , 1629-33, (2010) Midazolam is an ultra short acting benzodiazepine derivative and a specific probe for phenotyping cytochrome P450 (P450) 3A4/5 activity. A rapid, sensitive, and selective LC–MS/MS method was developed for simultaneous quantitation of midazolam and its metabol... |
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Determination of midazolam and its major metabolite 1'-hydroxymidazolam by high-performance liquid chromatography-electrospray mass spectrometry in plasma from children.
J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 821(1) , 1-7, (2005) We have developed a sensitive, selective and reproducible reversed-phase high-performance liquid chromatography method coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS) for the simultaneous quantification of midazolam (MDZ) and its major me... |
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Rapid and simultaneous measurement of midazolam, 1'-hydroxymidazolam and digoxin by liquid chromatography/tandem mass spectrometry: application to an in vivo study to simultaneously measure P-glycoprotein and cytochrome P450 3A activity.
J. Pharm. Biomed. Anal. 55(1) , 187-93, (2011) In order to simultaneously determine in vivo P-glycoprotein (P-gp) and Cytochrome P450 3A (CYP3A) activity, a new, rapid and sensitive liquid chromatography/tandem mass spectrometry (LC-MS/MS) method has been developed and fully validated to simultaneously de... |
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Determination of midazolam and 1-hydroxymidazolam from plasma by gas chromatography coupled to methane negative chemical ionization mass spectrometry after sublingual administration of midazolam.
J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 879(19) , 1668-76, (2011) A sensitive and selective gas chromatographic mass spectrometric method for the determination of midazolam and its biologically active metabolite, 1-hydroxymidazolam, in rabbit plasma has been developed and validated. Sample preparation includes mixed-mode so... |
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Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity.
Eur. J. Clin. Pharmacol. 69(3) , 507-13, (2013) The aim of this clinical study was to investigate a previously proposed mechanism of ketoconazole-mediated inhibition of cytochrome P450 3A (CYP3A) induction.A two-phase, randomized, cross-over, open, mono-centre trial was carried out. Participants received k... |