| 新型5-HT2A选择性配体N-取代哌啶-4-苯硫醚和砜类衍生物的合成及其生物活性 |
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| 引用本文： | 王浩,闻韧,黄磊,Robert B.Innis,谈平中.新型5-HT2A选择性配体N-取代哌啶-4-苯硫醚和砜类衍生物的合成及其生物活性[J].药学学报,2001,36(4):274-277. |
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| 作者姓名： | 王浩 闻韧 黄磊 Robert B.Innis 谈平中 |
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| 作者单位： | 1. 复旦大学药学院
2. 耶鲁大学医学院 WH CT 06516 美国 |
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| 基金项目： | 国家自然科学基金资助项目! (2 9872 0 2 9) |
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| 摘 要： | 目的为寻找新型的5-HT2A受体选择性配体,设计合成了一系列二芳烷基哌啶类化合物的含硫衍生物。方法以2，3-二甲氧基硫酚为原料，经烃化、氧化和水解等反应合成3个N-取代哌啶-4-苯硫醚和砜类化合物,所有目标化合物结构均经元素分析、1HNMR谱、质谱和红外光谱确证,并测定其对5-HT2A，5-HT2C，5-HT6和5-HT7受体及其他一些中枢神经递质受体的体外亲和力。结果3个目标化合物(2a-2c)及5个中间体均为新化合物。体外受体竞争结合试验结果表明2a-2c均有较高的5-HT2A受体选择性。结论此类化合物对5-HT2A受体的选择性较高,值得进一步研究。
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| 关 键 词： | 5-HT2A受体 选择性配体 4-(2 3-二甲氧苯硫基)-N-4-氟苯乙基哌啶 砜类衍生物 |
| 收稿时间： | 2000-09-05 |
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW 5-HT2A SELECTIVE LIGANDS N-SUBSTITUTED-PIPERIDINYL4-PHENYLTHIOETHER AND SULFONE DERIVATIVES |
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| WANG Hao,WEN Ren,HUANG Lei,Robert B.Innis,TAN Ping-zhong.SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW 5-HT2A SELECTIVE LIGANDS N-SUBSTITUTED-PIPERIDINYL4-PHENYLTHIOETHER AND SULFONE DERIVATIVES[J].Acta Pharmaceutica Sinica,2001,36(4):274-277. |
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| Authors: | WANG Hao WEN Ren HUANG Lei Robert BInnis TAN Ping-zhong |
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| Institution: | Department of Medicinal Chemistry of Fudan University, Shanghai 200032, China. |
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| Abstract: | AIM A series of 4-piperidinylthioether and sulfone derivatives of 4-1-hydroxy-1-(2,3-dimethoxyphenyl) methyl]- N -2-(4-fluorophenylethyl) piperidine (MDL 100907) were synthesized in order to find new 5-HT 2A selective ligands. METHODS Title compounds 2a-2c were synthesized from 2,3-dimethoxythiophenol and tested for their affinities to 5-HT 2A , 5-HT 2C , 5-HT 6 and 5-HT 7 receptors and some other nervous transmitter receptors in vitro . RESULTS Compounds 2a-2c are new compounds. The results of the binding assay demonstrated that they have relatively high selectivity for 5-HT 2A receptor in vitro . CONCLUSION Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT 2A receptor and are worth further study. |
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| Keywords: | 5-HT_(2A) receptor selective ligand 4-[1-hydroxy-1-(2 3-dimethoxyphenyl) methyl]- N -2-(4-fluorophenylethyl) piperidine sulfone derivative |
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