| 二氢吡啶载体介导的他克林前体药物合成及靶向性研究 |
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| 引用本文： | 瞿鼎,杨铁虹,张邦乐,宦梦蕾,梅其炳. 二氢吡啶载体介导的他克林前体药物合成及靶向性研究[J]. 中国新药杂志, 2010, 0(2) |
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| 作者姓名： | 瞿鼎 杨铁虹 张邦乐 宦梦蕾 梅其炳 |
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| 作者单位： | 第四军医大学药学系药理教研室; |
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| 基金项目： | 国家自然科学基金(30400548) |
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| 摘 要： | 目的:合成以他克林(THA)为原药的化学传输系统,证实其有脑靶向性。方法:将THA与氯乙酰氯连接,再与烟酰胺成季胺盐,最后将其还原成二氢吡啶载体介导的前体药物。结果:用NMR,MS等方法对前药进行结构表征鉴定。前药分子脂溶性比THA大,体内外实验各组织药物浓度监测显示脑组织匀浆浓度高于其他组织匀浆。结论:合成的二氢吡啶载体介导的前体药物脑内药物浓度高于外周,预示着有良好的脑靶向性。
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| 关 键 词： | 脑靶向 他克林 脂溶性 二氢吡啶载体介导前药 高效液相色谱 |
Synthesis and targeting of dihydropyridine carrier-mutual prodrug of tacrine |
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| QU Ding,YANG Tie-hong,ZHANG Bang-le,HUAN Meng-lei,MEI Qi-bing. Synthesis and targeting of dihydropyridine carrier-mutual prodrug of tacrine[J]. Chinese Journal of New Drugs, 2010, 0(2) |
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| Authors: | QU Ding YANG Tie-hong ZHANG Bang-le HUAN Meng-lei MEI Qi-bing |
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| Affiliation: | QU Ding,YANG Tie-hong,ZHANG Bang-le,HUAN Meng-lei,MEI Qi-bing (Department of Pharmacology,the Fourth Military Medical University,Xi'an 710032,China) |
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| Abstract: | Objective:To synthesize a chemical delivery system of tacrine(THA) in order to improve its brain targeting.Methods: THA was linked with chloroacetyl chloride,and then with nlcotlnamide.Finally pyridine quaternary ammonium was deoxidized to form the dihydropyridine carrier-mutual prodrug.Results: The structure of the prodrug was determined by NMR and MS.The lipophilicity of prodrug was increased as compared with THA.The drug concentrations were higher in brain homogenates than in other tissue homogenates in ... |
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| Keywords: | brain-targeting tacrine lipophilicity dihydropyridine carrier-mutual prodrug HPLC |
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