Bercher H, Grisk A
Acta Biol Med Ger. 1975;34(4):667-74.
10 compounds from the 2.4- and 3.4-difluorinated phenylethanol-amines series were tested for their antagonistic action against a hyperglycemia induced by catecholamines in rats, and the ED50 and AD50 values were determined. All the substances acted beta-adrenolytically, with the glycogenolysis enhanced by isoproterenol being blocked more potently by 3.4-difluorophenylethanolamines than by the corresponding 2.4-difluoroderivatives. An exception in the series is 2.4-difluoro-n-butylnoradrenalin, which acts 10fold more beta-adrenolytically than the 3.4-difluoroderivative, and has 3 times the effect of the comparative substance dichloroisoproterenol.
对2,4-二氟苯乙醇胺系列和3,4-二氟苯乙醇胺系列中的10种化合物进行了测试,以检测它们对大鼠体内儿茶酚胺诱导的高血糖的拮抗作用,并测定了半数有效剂量(ED50)和半数致死剂量(AD50)值。所有物质均表现出β-肾上腺素能阻断作用,异丙肾上腺素增强的糖原分解作用被3,4-二氟苯乙醇胺比相应的2,4-二氟衍生物更有效地阻断。该系列中的一个例外是2,4-二氟正丁基去甲肾上腺素,其β-肾上腺素能阻断作用比3,4-二氟衍生物强10倍,且其效果是对照物质二氯异丙肾上腺素的3倍。