Vasorelaxant activity of phthalazinones and related compounds

被引：64
作者：
del Olmo, E [1 ]
Barboza, B
Ybarra, MI
López-Pérez, JL
Carrón, R
Sevilla, MA
Boselli, C
Feliciano, AS
机构：
[1] Univ Salamanca, Fac Farm, CISET, Dept Quim Farmaceut, E-37007 Salamanca, Spain
[2] Univ Nacl Tucuman, Fac Bioquim Quim & Farm, San Miguel De Tucuman, Argentina
[3] Univ Salamanca, Fac Farm, Dept Fisiol & Farmacol, E-37007 Salamanca, Spain
[4] Univ Pavia, Fac Farm, Dept Farmacol, I-27100 Pavia, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期
关键词：
dihydrostilbenamide; phthalazinone; vasorelaxant activity; Rat aorta rings; alpha(1A); alpha(1B) and alpha(1D) sub-receptors affinity;
D O I：
10.1016/j.bmcl.2006.02.003
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Several series of dihydrostilbenamide, imidazo[2,1-a]isoindole, pyrimido[2,1-a]isoindole and phthalazinone derivatives were obtained and their vasorelaxant activity was measured on isolated rat aorta rings pre-contracted with phenylephrine (10(-5) M). Some phthalazinones attained, practically, the total relaxation of the organ at micromolar concentrations. For the most potent compound 9h (EC50 = 0.43 mu M) the affinities for alpha(1A), alpha(1B) and alpha(1D) adrenergic sub-receptors were determined. (C) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2786 / 2790
页数：5
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