Skowroński R, Madrala A, Angielski S
Acta Biochim Pol. 1984;31(2):251-62.
The effect of oral hypoglycaemic drugs, SPC-703 [n-(p-toluenesulphonyl)-5-methyl-2-pirazoline-1-carbonami de] and tolbutamide on insulin binding by rat adipocytes from epididymal fat pads were studied. SPC-703 and tolbutamide in concentration of 1 mM added in vitro to the suspension of adipocytes had no effect on insulin binding and kinetic parameters of insulin receptors. Daily administration of 300 mg/kg body weight of SPC-703 or tolbutamide for 10 days resulted in 48% and 34% increase of specific binding of insulin by adipocytes, respectively. From the Scatchard plot it appears that the increase of binding resulted from increased affinity of insulin receptors. These results may explain extrapancreatic action of sulphonylurea derivatives.
研究了口服降糖药SPC - 703 [N -（对甲苯磺酰基）- 5 -甲基- 2 -吡唑啉- 1 -碳酰胺]和甲苯磺丁脲对来自附睾脂肪垫的大鼠脂肪细胞胰岛素结合的影响。体外向脂肪细胞悬液中加入浓度为1 mM的SPC - 703和甲苯磺丁脲，对胰岛素结合及胰岛素受体的动力学参数均无影响。每日按300 mg/kg体重给予SPC - 703或甲苯磺丁脲，连续给药10天，结果脂肪细胞对胰岛素的特异性结合分别增加了48%和34%。从Scatchard图来看，结合增加似乎是由于胰岛素受体亲和力增加所致。这些结果可能解释了磺酰脲类衍生物的胰腺外作用。
