Galitzky J, Carpéné C, Bousquet-Mélou A, Berlan M, Lafontan M
Inserm U317, Laboratoire de Pharmacologie Médicale et Clinique, Faculté de Médecine, Toulouse France.
Fundam Clin Pharmacol. 1995;9(4):324-31. doi: 10.1111/j.1472-8206.1995.tb00506.x.
This review summarizes the experiments performed by various groups to determine how the activation of the different beta-adrenoceptors (beta-ARs) is ordinated when they are present in the same fat cell and involved in the same biological event. When expressed after the transfection of their genes in Chinese hamster ovary cell (CHO cells), beta 1- and beta 2-ARs present a higher affinity for catecholamines than beta 3-ARs. In vitro, the lipolytic effect induced by low concentrations of catecholamines in dog and rat white fat cells is due to the selective activation of beta 1- and/or beta 2-ARs. Higher concentrations only are able to activate beta 3-ARs. Similar results have been obtained in rat brown adipocytes. On the other hand, the lipolytic effect of catecholamines in human and primate adipocytes does not involve a beta 3-AR component whatever the concentration used. In vivo experiments in the dog have also shown that lipomobilization induced by low doses of isoprenaline only involved beta 1- and beta 2-AR activation, this effect being blocked by beta 1-/beta 2-antagonist pretreatment. However, in the same blockade conditions, perfusion of a 10-fold higher dose of isoprenaline revealed a beta 3-AR contribution in the lipomobilizing effect. These data showed that brown and white adipocyte beta 3-ARs possess a lower affinity for catecholamines than beta 1- and beta 2-ARs and are only recruited by high concentrations of the amines.(ABSTRACT TRUNCATED AT 250 WORDS)
本综述总结了不同研究小组所进行的实验,以确定当不同的β-肾上腺素能受体(β-ARs)存在于同一脂肪细胞并参与同一生物学事件时,它们的激活是如何协调的。当β1-和β2-ARs基因在中国仓鼠卵巢细胞(CHO细胞)中转染后表达时,它们对儿茶酚胺的亲和力高于β3-ARs。在体外,低浓度儿茶酚胺在犬和大鼠白色脂肪细胞中诱导的脂解作用是由于β1-和/或β2-ARs的选择性激活。只有更高的浓度才能激活β3-ARs。在大鼠棕色脂肪细胞中也得到了类似的结果。另一方面,无论使用何种浓度,儿茶酚胺在人和灵长类动物脂肪细胞中的脂解作用都不涉及β3-AR成分。犬的体内实验还表明,低剂量异丙肾上腺素诱导的脂肪动员仅涉及β1-和β2-AR的激活,这种作用可被β1-/β2-拮抗剂预处理所阻断。然而,在相同的阻断条件下,灌注高10倍剂量的异丙肾上腺素显示β3-AR在脂肪动员作用中有贡献。这些数据表明,棕色和白色脂肪细胞中的β3-ARs对儿茶酚胺的亲和力低于β1-和β2-ARs,并且只有在高浓度胺类的情况下才会被激活。(摘要截短于250字)