Synthesis and 5-HT2A, 5-HT1Aand α1-Binding Affinities of 2-[2-Hydroxy-3-(pyridin-3-yl-methyl)amino]-, 2-[2-Hydroxy-3-(2-pyridin-2-yl-ethyl)amino]- and 2-[2-Hydroxy-3-(4-N-methyl-piperazin-1-yl)-amino]propoxybenzaldehyde-O-(substituted) Benzyl Oximes
作者:Elisabetta Orlandini、Simona Rapposelli、Susanna Nencetti、Gino Giannaccini、Laura Betti、Aldo Balsamo
DOI:10.1002/ardp.200600123
日期:2007.3
Some oxime ether‐substituted aryloxypropanolamines 3‐5, structurally related to the active metabolite 2 of sarpogrelate 1, were synthesized and tested for their affinities at 5‐HT2A and 5‐HT1A serotoninergic receptors as well as at the α1‐adrenoceptor. The results show that the compounds possess, at least partially, the ability of the model compounds 1 and 2 to interact with the 5‐HT2A‐receptors; they
合成了一些肟醚取代的芳氧基丙醇胺 3-5,在结构上与沙格雷酯 1 的活性代谢物 2 相关,并测试了它们对 5-HT2A 和 5-HT1A 5-羟色胺能受体以及 α1-肾上腺素受体的亲和力。结果表明,这些化合物至少部分具有模型化合物 1 和 2 与 5-HT2A-受体相互作用的能力;它们对 5-HT2A 受体与 α1-肾上腺素受体具有相同的选择性。