Kobayashi S, Naitoh T, Nakadate T, Kimura I, Kimura M
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
J Pharmacobiodyn. 1992 Apr;15(4):175-80. doi: 10.1248/bpb1978.15.175.
The specific binding of insulin to diaphragm and flexor digitorum brevis (FDB) muscles isolated from diabetic KK-CAy and streptozotocin (STZ)-diabetic ddY mice was investigated under high glucose concentration in vitro. For high-affinity insulin receptor under 2.8 mM glucose, amounts of the receptor and values of dissociation constant (Kd) were greater in both diabetic muscles than in the corresponding normal control muscles, respectively. High glucose concentration up to 16.7 mM reduced both the up-regulation of the receptor and the decrease in the affinity by the diabetic state. These studies strongly suggest that high glucose level in the diabetic state in vivo may suppress the up-regulation of high-affinity insulin receptor in both models of diabetic mice.
在体外高葡萄糖浓度条件下,研究了胰岛素与从糖尿病KK-CAy小鼠和链脲佐菌素(STZ)诱导的糖尿病ddY小鼠分离的膈肌和趾短屈肌(FDB)的特异性结合。对于2.8 mM葡萄糖浓度下的高亲和力胰岛素受体,两种糖尿病肌肉中的受体数量和解离常数(Kd)值分别高于相应的正常对照肌肉。高达16.7 mM的高葡萄糖浓度减少了糖尿病状态引起的受体上调和亲和力降低。这些研究强烈表明,体内糖尿病状态下的高血糖水平可能会抑制两种糖尿病小鼠模型中高亲和力胰岛素受体的上调。