Amlaiky N, Leclerc G
J Pharm Sci. 1985 Oct;74(10):1117-9. doi: 10.1002/jps.2600741024.
1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal muscle and left atrium but retained high beta 1-selectivity. Irreversible beta-adrenoceptor antagonism of 8 was assessed by the blockade of the isoproterenol response of the guinea pig atria and by ligand binding studies with rat cerebral cortex.
合成了1-[4-(2-环丙基甲氧基乙基)苯氧基]-3-[1-p-(溴乙酰氨基苯基)-2-甲基-2-丙胺]-2-丙醇(8)，它是β1-肾上腺素能药物倍他洛尔的衍生物。在豚鼠气管平滑肌和左心房的体外试验中，化合物8的β-肾上腺素能阻断活性比倍他洛尔弱，但仍保持高β1选择性。通过豚鼠心房异丙肾上腺素反应的阻断以及大鼠大脑皮层的配体结合研究评估了8的不可逆β-肾上腺素能受体拮抗作用。
