CAS: 192876-02-1; (E)-5-Hydroxy-1-(4-(Trifluoromethyl)Phenyl)Pentan-1-One O-(2-Aminoethyl) Oxime

上下游产品

fluvoxamine maleate

📜马来酸氟伏沙明置于reconstituted Human Liver Microsomes Glucose-6-Phosphate Dehydrogenase,α-D-吡喃葡萄糖6-磷酸,Nicotinamide Adenine Dinucleotide Phosphate体系中,用 Phosphate Buffer 用作溶剂,化学反应 0.5H,反应生成(5E)-5-[(2-氨基乙氧基)亚氨基]-5-[4-(三氟甲基)苯基]-1-戊醇
参考文献:Identification Of Human Cytochrome P450 Enzymes Involved In The Major Metabolic Pathway Of Fluvoxamine
标题:Identification Of Human Cytochrome P450 Enzymes Involved In The Major Metabolic Pathway Of Fluvoxamine
摘要:The Metabolism Of Fluvoxamine To Fluvoxamino Acid Is Known To Involve A Two-Step Oxidation Process Via An Alcohol Intermediate,Fluvoxamino Alcohol. The Present Study Was Carried Out To Identify The Cytochrome P450 (Cyp) Enzyme(S) Involved In The Metabolism Of Fluvoxamine To Fluvoxamino Alcohol Using Human Liver Microsomes And Cdna-Expressed Human Cyp Enzymes. The Mean Km And Vmax Values For The Formation Of Fluvoxamino Alcohol From Fluvoxamine In Human Liver Microsomes Were 76.3 Mu M And 37.5 Pmol Min(-1) Mg(-1) Protein,Respectively. The Formation Of Fluvoxamino Alcohol From Fluvoxamine In Pooled Human Liver Microsomes Was Significantly Inhibited By Quinidine,A Relatively Specific Cyp2D6 Inhibitor,With A K-I Value Of 2.2 Mu M,Whereas Other Several Relatively Specific Cyp Inhibitors Did Not Inhibit The Formation Of Fluvoxamino Alcohol. In Addition,Only Cyp2D6 Of Several Cdna-Expressed Human Cyp Enzymes Examined Showed Substantial Activity For The Formation Of Fluvoxamino Alcohol. Furthermore,The Formation Of Fluvoxamino Acid From Fluvoxamino Alcohol Is Potently Inhibited By 4-Methylpyrazole In Human Liver Cytosol. These Data Suggest That Cyp2D6 Is The Only Enzyme Predominantly Responsible For The First-Step Oxidation Of Fluvoxamine To Fluvoxamino Alcohol,And Alcohol Dehydrogenase Is Involved In The Second-Step Oxidation Of Fluvoxamino Alcohol To The Corresponding Carbolic Acid.
Doi:10.1080/00498250600718464

专利信息

专利号:CN-108484624-A
优先权日:2018-05-21
标 题 :A kind of irinotecan hydrochloride impurity and its synthesis method and application