Gregorio F, Ambrosi F, Filipponi P, Cristallini S, Santeusanio F
Dipartimento di Medicina Clinica, Patologia e Farmacologia, Universitá degli Studi di Perugia, Italy.
J Diabetes Complications. 1994 Oct-Dec;8(4):204-12. doi: 10.1016/1056-8727(94)90045-0.
This study compares the insulin-secretory profiles induced by therapeutical concentrations of four different sulfonylureas--tolbutamide, gliquidone, gliclazide, and glibenclamide--and the amount of hormone released by each under different ambient glucose concentrations, using the isolated perfused rat pancreas model. All four sulfonylureas stimulated B-cell function, but the kinetics varied. Tolbutamide, gliquidone, and gliclazide produced a quick, biphasic release, whereas glibenclamide stimulated a delayed monophasic insulin secretion. Dramatic falls in insulin release were observed when ambient glucose concentrations were lowered. Glucagon release was not influenced by any of the sulfonylureas whatever the metabolic condition, neither directly nor indirectly, via an insulin-mediated paracrine inhibition of A-cell activity.
本研究使用离体灌注大鼠胰腺模型，比较了四种不同磺脲类药物（甲苯磺丁脲、格列喹酮、格列齐特和格列本脲）治疗浓度诱导的胰岛素分泌曲线，以及在不同环境葡萄糖浓度下每种药物释放的激素量。所有四种磺脲类药物均刺激B细胞功能，但动力学有所不同。甲苯磺丁脲、格列喹酮和格列齐特产生快速的双相释放，而格列本脲刺激延迟的单相胰岛素分泌。当环境葡萄糖浓度降低时，观察到胰岛素释放急剧下降。无论代谢状况如何，胰高血糖素的释放均不受任何磺脲类药物的直接或间接影响，即通过胰岛素介导的旁分泌抑制A细胞活性。
