CAS: 174756-45-7; 2-Hydroxymethylolanzapine

上下游产品

1-methyl-piperazine (10-Amino-4H-3-thia-4,9-diaza-benzo[f]azulen-2-yl)-methanol 2-amino-3-cyanothiophene ortho-nitrofluorobenzene

📜奥氮平置于α-D-吡喃葡萄糖6-磷酸,Glucose Phosphate Dehydrogenase,Human Cytochrome P450 (Cyp) 2D6.1,Recombinant,烟酰胺腺嘌呤双核苷酸磷酸盐体系中,用 Aq. Phosphate Buffer 用作溶剂,化学反应 0.75H,反应生成[4-(4-甲基-1-哌嗪基)-10H-噻吩并[2,3-B][1,5]苯并二氮杂卓-2-基]甲醇
参考文献:抗精神病药物olanzapine与非吸烟和吸烟日本受试者在细胞色素p4502D6和含黄素的单加氧酶3基因型上的体外和体内代谢清除率存在个体差异.
标题:抗精神病药物olanzapine与非吸烟和吸烟日本受试者在细胞色素p4502D6和含黄素的单加氧酶3基因型上的体外和体内代谢清除率存在个体差异.
摘要:目的据报道,抗精神病药物奥氮平通过不同途径被诱导型人细胞色素p450(cyp)1A2和可变拷贝数cyp2D6以及多态性含黄素单加氧酶3(fmo3)代谢.我们调查了体内和体外奥氮平代谢物形成和清除的个体差异.方法对21例日本人的cyp2D6基因型(平均年龄:50岁,范围:32-69岁,男14例,女7例,包括6名吸烟者)进行人肝微粒体olanzapine氧化活性的测定,并测定血浆olanzapine的浓度. 1,* 5和* 10)和fmo3(e158K,C197Fsx,R205C,V257M,E308G和r500X).结果呋喃西林(一种cyp1A2抑制剂),奎尼丁(一种cyp2D6抑制剂),热处理(使fmo3失活)可使奥氮平的肝微粒体代谢清除率降低约30%.在使用肝微粒体和重组酶的实验中,发现奥氮平的n-去甲基化和n-加氧分别由cyp1A2和cyp2D6以及cyp2D6和fmo3催化.血浆浓度
Doi:10.1002/hup.2515

专利信息

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:WO-2009035652-A1
优先权日:2007-09-13
标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

专利号:US-2014336387-A1
优先权日:2007-09-13
标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof

专利号:EP-2727915-A1
优先权日:2007-09-13
标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof

专利号:CA-2698808-A1
优先权日:2007-09-13
标题:Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof

专利号:EP-2200997-A1
优先权日:2007-09-13
标 题:Synthesis of deuterated catechols and benzoýd¨ý1,3¨dioxoles and derivatives thereof