Wenkeová J, Kuhn E, Wenke M
Eur J Pharmacol. 1975 Jan;30(1):49-55. doi: 10.1016/0014-2999(75)90201-0.
In human adipose tissue in vitro, dose-response curves of lipolytic agents in releasing free fatty acids and glycerol into an albumine-containing medium were followed. Norepinephrine and adrenaline produced about 20% of the maximal effect of isoproterenol, isopropylnorsynephrine about 40%, theophylline more than 100%. Found pD2 values were approximately 7.4 for isoproterenol and norepinephrine, approximately 5.9 for isopropylnorsynephrine. Phentolamine (1 times 10-5 M) elevated the maximal norepinephrine effects up to the isoproterenol maxima. Phenoxybenzamine (1 times 10-5 M) had significantly lower potentiating effects. Phenylephrine depressed lipolytic actions of isoproterenol (1 times 10-6 M) showing the same pI2 value 3.0 as well in human as in rat adipose tissue and exerted per se weak lipolytic effects also. It is concluded neither potentiating actions of alpha-blockers nor depressing effects of phenylephrine in human adipose tissue seem related to affecting adrenergic alpha-receptors. The existence of antilipolytic actions of adrenergic alpha-receptors is questioned.
在人体脂肪组织的体外实验中,追踪了脂解剂在向含白蛋白的培养基中释放游离脂肪酸和甘油时的剂量 - 反应曲线。去甲肾上腺素和肾上腺素产生的最大效应约为异丙肾上腺素的20%,异丙去甲肾上腺素约为40%,茶碱超过100%。测得异丙肾上腺素和去甲肾上腺素的pD2值约为7.4,异丙去甲肾上腺素约为5.9。酚妥拉明(1×10⁻⁵ M)将去甲肾上腺素的最大效应提高到异丙肾上腺素的最大值水平。酚苄明(1×10⁻⁵ M)的增强作用明显较低。去氧肾上腺素抑制异丙肾上腺素(1×10⁻⁶ M)的脂解作用,在人体和大鼠脂肪组织中显示出相同的pI2值3.0,并且其本身也具有较弱的脂解作用。得出的结论是,α受体阻滞剂在人体脂肪组织中的增强作用和去氧肾上腺素的抑制作用似乎都与影响肾上腺素能α受体无关。对肾上腺素能α受体抗脂解作用的存在提出了质疑。