CAS: 2558-30-7; N-Desmethylflunitrazepam

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CAS号1622-62-4 氟硝西泮 | CAS号344-80-9 2-氨基-5-硝基-2''-氟二苯甲酮

📜氟硝西泮置于human Hepatocytes,Williams' Medium E Cell Culture Medium体系中,用 乙腈 用作溶剂,化学反应 1.0H,反应生成5-(2-氟苯)-7-硝基-1,3-二水-2H-1,4-苯并氮杂卓-2-酮
参考文献:Prediction Of Metabolic Clearance Using Fresh Human Hepatocytes: Comparison With Cryopreserved Hepatocytes And Hepatic Microsomes For Five Benzodiazepines
标题:Prediction Of Metabolic Clearance Using Fresh Human Hepatocytes: Comparison With Cryopreserved Hepatocytes And Hepatic Microsomes For Five Benzodiazepines
摘要:1. Predictions Of In Vivo Intrinsic Clearance From Cryopreserved Human Hepatocytes May Be Systematically Low. In The Current Study,The Metabolite Kinetics Of A Series Of Cyp3A4 Substrates (Benzodiazepines) In Fresh Human Hepatocytes From Five Donors,Via A Major Uk Supplier,Were Investigated And Compared With Those Previously Reported (By The Authors' Laboratory) For Cryopreserved Human Hepatocytes And Hepatic Microsomes.2. A High Incidence Of Autoactivation (Up To Tenfold) And Heteroactivation (By Testosterone,Up To 14-Fold) Among The Major Pathways Was Observed. Cyp Capacity (V-Max) Was Marginally Lower And 'Affinity' Constants (K-M,S-50) Were Marginally Greater Compared With Cryopreserved Hepatocytes.3. Average Intrinsic Clearance (Based On Maximal Clearance,Clmax) Was Sevenfold Lower Than In Cryopreserved Hepatocytes (Reflecting Sensitivity Of Intrinsic Clearance Estimation In Vitro To Mechanistic Parameter Values,Particularly Those Involving Atypical Kinetics),But Scaled Intrinsic Clearances For Fresh (And Cryopreserved) Hepatocytes Were Within The Range Previously Determined In Hepatic Microsomes.4. There Was No Evidence From This Series Of Studies That Fresh Hepatocytes Provide Quantitatively Improved Estimates Of Intrinsic Clearance Over Cryopreserved Hepatocytes.
Doi:10.1080/00498250701834665

专利信息

专利号:US-4118386-A
优先权日:1977-04-04
标 题:Synthesis of imidazo[1,5-a]diazepine-3-carboxylates
发明人：WALSER ARMIN
权利人:HOFFMANN LA ROCHE
摘要:A process to produce diazepine-3-carboxylates of the formula ##STR1## is selected from the group consisting of ##STR2## R 6 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, and lower alkanoyl; n R 4 is lower alkyl; R 3 is selected from the group consisting of phenyl, mono-substituted phenyl, disubstituted phenyl, pyridyl and mono-substituted pyridyl; and R 2 is hydrogen or lower alkyl which comprises reacting a compound of the formula ##STR3## wherein R 1 is of the formula ##STR4## AND R 5 is lower alkyl with a compound of the formula n n Nâ•?C-CH.sub.2 --COOR.sub.4 n n in the presence of a base sufficiently strong to generate the anion of the isocyanoacetate.