Schmid-Antomarchi H, de Weille J, Fosset M, Lazdunski M
Biochem Biophys Res Commun. 1987 Jul 15;146(1):21-5. doi: 10.1016/0006-291x(87)90684-x.
The ATP-sensitive K+ channel of RINm5F insulinoma cells is activated after an intracellular ATP depletion. This activation can be followed by 86Rb+ efflux. Once activated by ATP depletion, the K+ channel can be blocked by the hypoglycemic drug, glibenclamide. The blockade is of a high-affinity type (K0.5 = 0.06 nM). Recording of the activity of ATP-sensitive K+ channels with the patch-clamp technique confirmed that they could be completely blocked with 20 nM glibenclamide.
RINm5F胰岛素瘤细胞的ATP敏感性钾通道在细胞内ATP耗竭后被激活。这种激活可通过86Rb+外流来追踪。一旦被ATP耗竭激活,钾通道可被降血糖药物格列本脲阻断。这种阻断是高亲和力类型的(K0.5 = 0.06 nM)。用膜片钳技术记录ATP敏感性钾通道的活性证实,20 nM格列本脲可将其完全阻断。