Taouis M, Berlan M, Montastruc P, Lafontan M
Laboratoire de Pharmacologie Médicale, Faculté de Médecine, UA 644 Centre National de la Recherche Scientifique, Toulouse, France.
J Pharmacol Exp Ther. 1987 Sep;242(3):1041-9.
In the search of the most accurate animal model for studies on fat cell adrenoceptor regulation, the characterization of dog fat cell beta and alpha-2 adrenoceptor properties was carried out using selected radioligands and biological measurements of fat cell function. Moreover, the distribution of dog fat cell adrenoceptors and the functional consequences were explored in fat deposits from different anatomical locations (perirenal, omental and s.c. adipose tissue). Beta and alpha-2 adrenoceptors involved in the control of the lipolytic activity of dog fat cells exhibit pharmacological characteristics which are very similar to those defined in human adipocytes. However, in contrast with the results obtained in human adipocytes, there is a preponderance of beta over alpha-2 adrenergic binding sites, whatever the location of the fat deposits, in the dog. The higher values of the ratio beta-sites over alpha-2-sites were found in perirenal adipocytes whereas the lowest values of this ratio were found in s.c. deposits. A close positive relationship exist between alpha-2 adrenoceptor number, alpha-2 adrenergic responsiveness and fat cell volume. To conclude, beta and alpha-2 adrenoceptors exhibit similar pharmacological properties in dog and human fat cells. Variations according to the anatomical location of the fat deposits exist in both species. However, as opposed to human fat cells, it is evident that the balance between beta and alpha-2 adrenergic responsiveness is predominantly under the control of beta adrenoceptors in dog fat cells.
在寻找用于脂肪细胞肾上腺素能受体调节研究的最精确动物模型的过程中,利用选定的放射性配体和脂肪细胞功能的生物学测量方法,对犬脂肪细胞β和α-2肾上腺素能受体特性进行了表征。此外,还在不同解剖位置(肾周、网膜和皮下脂肪组织)的脂肪沉积物中探究了犬脂肪细胞肾上腺素能受体的分布及其功能后果。参与控制犬脂肪细胞脂解活性的β和α-2肾上腺素能受体表现出与人类脂肪细胞中所定义的药理学特性非常相似的特性。然而,与在人类脂肪细胞中获得的结果相反,在犬类中,无论脂肪沉积物位于何处,β肾上腺素能结合位点都比α-2肾上腺素能结合位点占优势。在肾周脂肪细胞中发现β位点与α-2位点的比率较高,而在皮下沉积物中发现该比率最低。α-2肾上腺素能受体数量、α-2肾上腺素能反应性与脂肪细胞体积之间存在密切的正相关关系。总之,β和α-2肾上腺素能受体在犬类和人类脂肪细胞中表现出相似的药理学特性。两种物种中脂肪沉积物的解剖位置不同,其特性也存在差异。然而,与人类脂肪细胞不同的是,显然在犬脂肪细胞中,β和α-2肾上腺素能反应性之间的平衡主要受β肾上腺素能受体的控制。