Maciag D, Filipek B, Czekaj T, Marona H, Nowak G
Department of Pharmacobiology, Faculty of Pharmacy, Medical College, Jagiellonian University, Kraków, Poland.
Pharmazie. 2003 Dec;58(12):899-905.
A series of aroxyethylamines (1-10) was synthesized and evaluated for hypotensive activity in rats after intravenous and oral administration. The 4 compounds (4, 7, 8 and 10) containing a (2-methoxy)phenylpiperazine moiety displayed hypotensive activity and their affinities for alpha1-, alpha2- and beta1-adrenoreceptors were determined by radioligand binding assays. Compounds 4, 7, 8 and 10 were also tested for their effect on the pressor responses to epinephrine, norepinephrine, methoxamine, tyramine and DMPP. The results suggest that the hypotensive effect of these compounds is related to their alpha- and beta-adrenolytic properties.
合成了一系列芳氧乙胺（1 - 10），并在大鼠静脉注射和口服给药后评估其降压活性。含有（2 - 甲氧基）苯基哌嗪部分的4种化合物（4、7、8和10）表现出降压活性，并通过放射性配体结合试验测定了它们对α1 -、α2 - 和β1 - 肾上腺素能受体的亲和力。还测试了化合物4、7、8和10对肾上腺素、去甲肾上腺素、甲氧明、酪胺和DMPP升压反应的影响。结果表明，这些化合物的降压作用与其α - 和β - 肾上腺素能阻断特性有关。
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