Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel K
ir6.2 (IC
50 = 4.3 nM).
1 It binds to microsomes derived from RINm5F pancreatic β-cells (K
d = 0.3 nM) and inhibits
86Rb
+ efflux from intact RINm5 cells with a half-maximal inhibition (K
0.5) value of 0.06 nM.
2 Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin (STZ; ).
3 It inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs).
4 Glyburide (80 mg/ml) also reduces lesion growth in mice infected with
L. mexicana.
5 Formulations containing glyburide have been used in the treatment of type 2 diabetes.
1. Coghlan, M.J., Carroll, W.A., and Gopalakrishnan, M. Recent developments in the biology and medicinal chemistry of potassium channel modulators: Update from a decade of progress J. Med. Chem. 44(11),1627-1653(2001).
2. Schmid-Antomarchi, H., De Weille, J., Fosset, M., et al. The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cells J. Biol. Chem. 262(33),15840-15844(1987).
3. Bugdayci, G., Altan, N., Sancak, B., et al. The effect of the sulfonylurea glyburide on glutathione-S-transferase and glucose-6-phosphate dehydrogenase in streptozotocin-induced diabetic rat liver Acta. Diabetol. 43(4),131-134(2006).
4. Lamkanfi, M., Mueller, J.L., Vitari, A.C., et al. Glyburide inhibits the Cryopyrin/Nalp3 inflammasome J. Cell Biol. 187(1),61-70(2009).
5. Serrano-Martín, X., Payares, G., and Mendoza-León, A. Glibenclamide, a blocker of K+ATP channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasis Antimicrob. Agents Chemother. 50(12),4214-4216(2006).
