Deleers M, Brasseur R
Pharmacol Res Commun. 1986 Feb;18(2):129-36. doi: 10.1016/0031-6989(86)90140-2.
The ability of glibenclamide and of gliclazide to act as protonophores has been studied in black lipid membranes made of glycerol monoleate as a function of pH and drug concentration. Protons may effectively be transported across lipid membranes with a maximum at a pH close to the pKa of the sulfamide (pKa of glibenclamide = 5.4). It is suggested therefore that hypoglycemic sulfonylureas may act in part as Ca2+ inward and H+ outward ionophores through plasma membranes of pancreatic B cells.
在以单油酸甘油酯制成的黑色脂质膜中，研究了格列本脲和格列齐特作为质子载体的能力，该能力是pH值和药物浓度的函数。质子可有效地跨脂质膜转运，在接近磺酰胺pKa（格列本脲的pKa = 5.4）的pH值时达到最大值。因此，有人提出，降血糖磺酰脲类药物可能部分通过胰岛B细胞膜作为Ca2+内向和H+外向离子载体起作用。
