CAS: 7143-09-1; Ecgonine Methyl Ester

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CAS号141120-39-0 methyl (1S,3S,4... | CAS号192648-66-1 methyl (3S,4R)-... | CAS号134507-62-3 4'-氟可卡因

📜古卡因置于human Carboxylesterase 2,Recombinant体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 1.0H,反应生成 芽子碱甲酯
参考文献:羧酸酯酶依赖性达比加群酯水解的鉴定.
标题:羧酸酯酶依赖性达比加群酯水解的鉴定.
摘要:达比加群酯 (Dabe) 是一种口服前药,可通过丝氨酸酯酶迅速转化为活性凝血酶抑制剂达比加群 (Dab).本研究的目的是研究人羧酸酯酶水解 Dabe 的体外动力学和途径,以及酒精对这些转化的影响.测定了两种人重组羧酸酯酶(ces1 和 Ces2)以及人肠道微粒体和人肝脏 S9 级分中 Dabe 水解的动力学.还检查了酒精(一种已知的 Ces1 抑制剂)对羧酸酯酶和人肝 S9 级分中 Dabe 代谢物形成的影响.研究了双(4-硝基苯基)磷酸酯对羧酸酯酶介导的 Dabe 代谢的抑制作用以及酒精对经典羧酸酯酶底物(可卡因)水解的影响,以验证体外模型.dabe 的乙酯仅被 Ces1 水解为 M1(km 24.9 +/-2.9 μm,Vmax 676 +/-26 Pmol/min 每毫克蛋白质),而 Dabe 的氨基甲酸酯仅被 Ces2 水解为 M2(km 5.5 +/-0.8 μm; Vmax 71.1
DOI:10.1124/dmd.113.054353

专利信息

专利号:US-6017541-A
优先权日:1994-06-13
标题 :Immunogens for the production of cocaine-hydrolyzing catalytic antibodies
发明人：BARBER BRIAN H; DEN HOLLANDER NEAL; KREPINSKY JIRI J; MEAH M YOUNUS
摘要:Methods are described for the rapid synthesis in satisfactory yield of methyl ecgonine phenylphosphonates as analogues of transition states for the hydrolysis of the benzoyl ester of an ecgonine derivative, namely cocaine, and their linking to carrier proteins, for the purpose of using them as immunogens. The resulting immunogens elicit the formation in experimental animals of antibodies able to promote the hydrolysis of cocaine. Both these catalytic anti-cocaine antibodies and the immunogens themselves are potentially useful for the treatment of individuals seeking to avoid the pharmacological effects of cocaine and in diagnostic applications.