一些拟肾上腺素药物在体外对人体脂肪组织的脂肪分解有影响。

Some adrenomimetic drugs affecting lipolysis in human adipose tissue in vitro.

作者信息

Wenkeová J, Kuhn E, Wenke M

出版信息

Eur J Pharmacol. 1976 Jan;35(1):1-6. doi: 10.1016/0014-2999(76)90294-6.

Abstract

In human adipose tissue in vitro, dose-response curves were followed for different adrenomimetics releasing free fatty acids and glycerol into an albumin-containing medium. Phenylephrine, salbutamol and t-butyl-norsynephrine produced lipolytic actions whose maximum did not exceed 20% of the maximal isoproterenol lipolysis. Phentolamine (1 x 10(-5) M) did not potentiate the effect of any of these drugs. When using salbutamol or t-butyl-norsynephrine for antagonizing isoproterenol actions, typical antagonism was found. The parallel shift of the isoproterenol curves showed pA2 values 5.8 for salbutamol and 5.7 for t-butyl-norsynephrine. Comparison of human and rat adipose tissue reactivity shows identical affinities of the drugs studied in both tissues, but related to isoproterenol, diminished intrinsic activities of salbutamol and t-butyl-norsynephrine in human adipose tissue.

摘要

在体外人脂肪组织中，对不同的肾上腺素能激动剂进行了剂量反应曲线研究，这些激动剂可将游离脂肪酸和甘油释放到含白蛋白的培养基中。去氧肾上腺素、沙丁胺醇和叔丁基去甲肾上腺素产生的脂解作用，其最大值不超过异丙肾上腺素最大脂解作用的20%。酚妥拉明（1×10⁻⁵M）不能增强这些药物中任何一种的作用。当使用沙丁胺醇或叔丁基去甲肾上腺素拮抗异丙肾上腺素的作用时，发现了典型的拮抗作用。异丙肾上腺素曲线的平行移动显示，沙丁胺醇的pA2值为5.8，叔丁基去甲肾上腺素的pA2值为5.7。人和大鼠脂肪组织反应性的比较表明，所研究的药物在两种组织中的亲和力相同，但与异丙肾上腺素相关，沙丁胺醇和叔丁基去甲肾上腺素在人脂肪组织中的内在活性降低。