Heseltine L, Webster J M, Taylor R
Human Metabolism Research Centre, Medical School, University of Newcastle upon Tyne, UK.
Mol Cell Biochem. 1995 Mar 23;144(2):147-51. doi: 10.1007/BF00944394.
The dose response effect of a new adenosine analogue, GR79236 (N-[1S trans-2-hydroxycyclopentyl] adenosine) upon insulin sensitivity was examined in human adipocytes. The influence of adenosine upon insulin sensitivity for suppression of lipolysis and stimulation of glucose transport was examined. Removal of adenosine by use of adenosine deaminase stimulated lipolysis to the same extent as did 10(-9) M noradrenaline. GR79236 brought about dose dependent inhibition of lipolysis with half-maximal effect at 11.3 +/- 7.8 x 10(-9) M. When lipolysis was stimulated by noradrenaline alone the subsequent inhibition of lipolysis brought about by GR79236 was significantly greater than that of insulin. To examine adenosine effects on the insulin signalling pathway separately from those on lipolysis, the insulin sensitivity of glucose transport was examined. Removal of adenosine brought about a small but significant increase in the concentration of insulin required for half-maximal stimulation of glucose transport. Adenosine agonists offer promise as new agents for the modulation of metabolism in diabetes and other states of insulin resistance.
在人脂肪细胞中研究了一种新的腺苷类似物GR79236(N-[1S反式-2-羟基环戊基]腺苷)对胰岛素敏感性的剂量反应效应。研究了腺苷对胰岛素抑制脂肪分解和刺激葡萄糖转运敏感性的影响。使用腺苷脱氨酶去除腺苷刺激脂肪分解的程度与10(-9) M去甲肾上腺素相同。GR79236引起脂肪分解的剂量依赖性抑制,半数最大效应浓度为11.3 +/- 7.8 x 10(-9) M。当仅由去甲肾上腺素刺激脂肪分解时,GR79236随后对脂肪分解的抑制作用明显大于胰岛素。为了分别研究腺苷对胰岛素信号通路的影响与对脂肪分解的影响,研究了葡萄糖转运的胰岛素敏感性。去除腺苷导致半数最大刺激葡萄糖转运所需的胰岛素浓度有小幅但显著的增加。腺苷激动剂有望成为调节糖尿病和其他胰岛素抵抗状态下代谢的新型药物。