中枢神经系统药物构效关系研究。第七部分。2-取代1-[3-(4-芳基-1-哌嗪基)丙基]咪唑中咪唑片段对其与5-HT1A和5-HT2受体相互作用模式的影响。

J L Mokrosz, B Duszyńska
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引用次数: 0

摘要

报道了2-取代咪唑(1-8)的合成及其对5-HT1A和5-HT2受体的亲和力。在生理条件下,N-3咪唑原子和N-1哌嗪原子都可以被认为是可能的质子化中心。发现1-8的折叠构象主要存在于溶液中。此外,所分析的化合物与5-HT1A和5-HT2受体位点的三种不同的相互作用模式已经被提出。
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Structure-activity relationship studies of CNS agents. Part VII. The effect of the imidazole fragment in 2-substituted 1-[3-(4-aryl-1-piperazinyl)propyl]imidazoles on their interaction modes with 5-HT1A and 5-HT2 receptors.

The synthesis and the 5-HT1A and 5-HT2 receptor affinity of 2-substituted 1-[3-(4-aryl-1-piperazinyl)propyl]-imidazoles (1-8) has been described. It has been shown that both the N-3 imidazole atom and the N-1 piperazine one should be considered as possible protonation centers under physiological conditions. It has been found that the folded conformations of 1-8 exist predominantly in solution. Moreover, three different modes of interaction of the analyzed compounds with 5-HT1A and 5-HT2 receptor sites have been proposed.

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