Iuzhakov S D, Zaĭtseva K A, Dorodnikova E V, Mashkovskiĭ M D
Farmakol Toksikol. 1985 May-Jun;48(3):36-40.
Some derivatives of 2-(3-amino-2-hydroxypropoxy)phenoxymethyl isoxazole possess beta- and alpha-adrenoblocking activity. 3-Methyl-4-chlor-5-(3-isopropylamino-2-hydroxypropoxy)phenoxymethyl isoxazole hydrochloride (compound OF-4452) is the most active of the compounds studied. As to the beta-adrenoblocking activity, this compound given in vivo and in vitro compares very favourably with propranolol, oxprenolol and labetalol, in particular; as regards the alpha-adrenoblocking action, it is not inferior to the latter drug. Compound OF-4452 has a partial agonist activity and nonspecific membrane-stabilizing action. It displays antifibrillatory and antiarrhythmic activity as well.
2-(3-氨基-2-羟基丙氧基)苯氧基甲基异恶唑的一些衍生物具有β-和α-肾上腺素能阻滞活性。3-甲基-4-氯-5-(3-异丙基氨基-2-羟基丙氧基)苯氧基甲基异恶唑盐酸盐(化合物OF-4452)是所研究化合物中活性最高的。就β-肾上腺素能阻滞活性而言,该化合物在体内和体外给予时,特别是与普萘洛尔、氧烯洛尔和拉贝洛尔相比,具有非常好的效果;就α-肾上腺素能阻滞作用而言,它不低于后一种药物。化合物OF-4452具有部分激动剂活性和非特异性膜稳定作用。它还表现出抗纤颤和抗心律失常活性。