Ribes G, Trimble E R, Blayac J P, Wollheim C B, Puech R, Loubatières-Mariani M M
Diabetologia. 1981 Apr;20(4):501-5. doi: 10.1007/BF00253415.
The effects of HB 699, a non-sulphonyl urea acyl-amino-alcyl benzoic acid derivative, were studied in unanesthetized dogs. Changes in blood glucose and plasma insulin, glucagon, pancreatic polypeptide and somatostatin were measured after a single intravenous injection. HB 699 caused hypoglycaemia and stimulated insulin secretion in a dose-dependent manner. The effects of HB 699 (40 mg/kg) on pancreatic hormone secretion were compared to those of tolbutamide give at a dose (12 mg/kg) which induced a similar maximal hypoglycaemia. Both drugs caused a similar increase in insulin release (180 +/- 32% for tolbutamide and 240 +/- 41% for HB 699) lasting for approximately 1 hour. Despite hypoglycaemia, plasma glucagon concentrations were unaltered by either substance. HB 699 caused a marked increase in the secretion of pancreatic polypeptide (220 +/- 60% at 30 min) for up to 2 hours, whereas tolbutamide caused no significant change in plasma pancreatic polypeptide levels. In contrast, while tolbutamide caused a significant (45 +/- 12%) but short-lived increase in plasma somatostatin concentrations, HB 699 had no significant effect.
在未麻醉的犬身上研究了非磺酰脲类酰基氨基烷基苯甲酸衍生物HB 699的作用。单次静脉注射后，测定血糖、血浆胰岛素、胰高血糖素、胰多肽和生长抑素的变化。HB 699可引起低血糖，并以剂量依赖的方式刺激胰岛素分泌。将HB 699（40mg/kg）对胰腺激素分泌的作用与甲苯磺丁脲（12mg/kg）的作用进行比较，后者可诱导相似的最大低血糖。两种药物均可使胰岛素释放产生相似的增加（甲苯磺丁脲为180±32%，HB 699为240±41%），持续约1小时。尽管出现低血糖，但两种物质均未改变血浆胰高血糖素浓度。HB 699可使胰多肽分泌显著增加（30分钟时为220±60%），持续长达2小时，而甲苯磺丁脲对血浆胰多肽水平无显著影响。相反，虽然甲苯磺丁脲可使血浆生长抑素浓度显著增加（45±12%），但持续时间较短，而HB 699无显著作用。
