Lee K, Ashford M L
Department of Pharmacology, University of Cambridge, UK.
Eur J Pharmacol. 1993 Nov 15;247(3):347-51. doi: 10.1016/0922-4106(93)90205-n.
Radioligand binding studies were performed to determine the effect of various cations on the characteristics of [3H]glibenclamide binding to its high-affinity receptor in rat cerebral cortex membranes. Mg2+ was shown specifically to reduce radioligand binding to membranes pretreated with 5 mM EDTA. CaCl2 enhanced [3H]glibenclamide binding whilst MnCl2, KCl and NaCl were without significant effect. 2 mM MgCl2 induced a statistically significant rightward shift in the dissociation constant for glibenclamide obtained from both saturation and competition studies. These results suggest that Mg2+ may participate in the regulation of the sulphonylurea receptor in the rat cerebral cortex.
进行放射性配体结合研究以确定各种阳离子对[3H]格列本脲与大鼠大脑皮层膜中其高亲和力受体结合特性的影响。结果显示，Mg2+能特异性降低与5 mM EDTA预处理过的膜的放射性配体结合。CaCl2增强了[3H]格列本脲的结合，而MnCl2、KCl和NaCl则无显著影响。2 mM MgCl2使从饱和研究和竞争研究中获得的格列本脲解离常数产生具有统计学意义的右移。这些结果表明，Mg2+可能参与大鼠大脑皮层中磺酰脲受体的调节。
