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河北医科大学药学院 Ziconotide(Prial0芋螺毒素 From Foe to Friend:Using Animal Toxins to Investigate Ion Channel Function 4,2004FD Venom of marine snails provide new drugs Ziconotide(Prialt)芋螺毒素 第五节C-15乙酸原化合物 1、直链C-15乙酸原化合物 冬结构特点:从EOAc成乙酰灿酶A生新合减,的 多分塞:1、直绿C15乙酸爱化合物 天然药化教研室史清文教授 河北医科大学药学院 天然药化教研室史清文教授 9 Cys-Lys-Gly-Lys-Gly-Ala-Lys-Cys-Ser-Arg-Leu-Met-Tyr-Asp-Cys-Cys-Thr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-Cys-NH2 Ziconotide (Prialt) Ziconotide (Prialt) 芋螺毒素 Ziconotide is the first N-type calcium-channel blocker and it is also the first marine-derived peptide drug on the market. Ziconotide is 1000-times more potent than morphine and it does not produce tolerance, which is well known with opiatebased therapies. Baldomero M. Olivera J. Michael McIntosh 1979 Isolated, 2004 FDA From Foe to Friend: Using Animal Toxins to Investigate Ion Channel Function 鸡心螺(Cone Snail)又叫“芋螺”、锥蜗牛,主要生长于热带海域,一般多 生活在暖海,属于软体动物门。Pain therapeutics from cone snail venoms: From Ziconotide to novel nonopioid pathways. Venom of marine snails provide new drugs Ziconotide was developed into an artificially manufactured drug by Elan Corporation. It was approved for sale under the name Prialt by the U.S. FDA on December 28, 2004, and by the European Commission on February 22, 2005. Their venom - and the way they deliver it - is the most interesting thing HO O N H NH S O HN O H N O N H O OH H N O N H O H2N OH O NH O S O NH HN S S N H H2N O NH2 NH O OH N H NH NH HN O O H2N O O O N H O OH H N O N H OH O HN O OH N H H N O O HO N H O HN O N H O HN O HN S S S NH2 O NH2 NH NH2 Baldomero M. Olivera J. Michael Mcintosh Ziconotide (Prialt) 芋螺毒素 世界著名神经药理 学家和海洋药物新 药研发专家、美国 犹他大学精神病学 系主任 第五节 C-15 乙酸原化合物 结构特点:从EtOAc 或乙酰辅酶A生物合成的 十五个碳的非萜类化合物。 主要来源于红藻的凹顶藻属Laurencia sp 分类: 1、 直链C-15 乙酸原化合物 OH 直链型 OH OH OH Laurencenyne  1、 直链C-15 乙酸原化合物 直链型
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