Izawa T, Komabayashi T, Suda K, Kunisada Y, Shinoda S, Tsuboi M
Laboratory for Exercise and Applied Physiology, Tokyo College of Pharmacy, Japan.
Res Commun Chem Pathol Pharmacol. 1988 May;60(2):253-6.
The effects of chronic administrations of isoproterenol (IPR) on adipocyte beta-adrenergic system were investigated. A 21-days in vivo administration of IPR (2.5 mg/kg BW/day) reduced (-)-IPR- and 5'-guanylylimidodiphosphate-stimulated adenylate cyclase activities. Moreover, the number of beta-adrenergic receptors (beta-AR) and (-)-IPR-stimulated [3H]GDP release from adipocyte membranes were significantly depressed in the treated rats compared to controls. These results suggest that the desensitized response of adenylate cyclase to beta-agonists, induced by chronic in vivo administrations of IPR, may result from impaired coupling efficiency between beta-AR and adenylate cyclase with the significant loss of the number of beta-AR and possible change(s) of guanine nucleotide regulatory proteins.
研究了长期给予异丙肾上腺素(IPR)对脂肪细胞β-肾上腺素能系统的影响。连续21天在体内给予IPR(2.5毫克/千克体重/天)可降低(-)-IPR和5'-鸟苷酰亚胺二磷酸刺激的腺苷酸环化酶活性。此外,与对照组相比,处理组大鼠脂肪细胞膜上β-肾上腺素能受体(β-AR)的数量以及(-)-IPR刺激的[3H]GDP释放均显著降低。这些结果表明,长期在体内给予IPR诱导的腺苷酸环化酶对β-激动剂的脱敏反应,可能是由于β-AR与腺苷酸环化酶之间的偶联效率受损,伴随着β-AR数量的显著减少以及鸟嘌呤核苷酸调节蛋白可能的变化所致。