Jorgensen K D
Acta Pharmacol Toxicol (Copenh). 1977 Feb;40(2):216-26.
The new sulphonylurea CS 476 has been shown to be a potent hypoglycaemic agent. In normal fasting dogs, rabbits, rats and mice the maximal hypoglycaemia produced by intravenous administration of CS 476 was comparable on a weight basis to that produced by glibenclamide. Randomized Latin square experiments in dogs showed that 0.03 mg/kg orally of CS 476 and of glibenclamide caused the same maximal decrease of blood glucose and that CS 476 had the shorter duration of action. CS 476 had no hypoglycaemic effect in totally pancreatectomized dogs nor in streptozotocin diabetic dogs and rats. The insulin releasing activity was studied in dogs after intravenous and oral administration of equipotent doses of CS 476, tolbutamide and glibenclamide. It was found that the insulin curves after CS 476 tended to have a plateau-like maximum like those after glibenclamide although the duration of effect was shorter.
新型磺酰脲类药物CS 476已被证明是一种强效降糖药。在正常禁食的犬、兔、大鼠和小鼠中,静脉注射CS 476产生的最大低血糖效应,按体重计算与格列本脲相当。犬的随机拉丁方实验表明,口服0.03 mg/kg的CS 476和格列本脲引起的血糖最大降幅相同,且CS 476的作用持续时间较短。CS 476对全胰腺切除的犬以及链脲佐菌素诱导的糖尿病犬和大鼠均无降糖作用。在犬静脉注射和口服等效剂量的CS 476、甲苯磺丁脲和格列本脲后,研究了它们的胰岛素释放活性。结果发现,CS 476后的胰岛素曲线虽然作用持续时间较短,但倾向于像格列本脲后的曲线那样有一个平台状的最大值。