Acetohexamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 ?M in HEK293 cells transfected with the human receptor and in rat brain, respectively.1 It is metabolized to the hypoglycemic compound L-hydroxyhexamide in vivo.2,3 Formulations containing acetohexamide have previously been used in the treatment of type 2 diabetes.
1.Gopalakrishnan, M., Molinari, E.J., Char-Change, S., et al.Pharmacology of human sulphonylurea receptor SUR1 and inward rectifier K+ channel Kir6.2 combination expressed in HEK-293 cellsBr. J. Pharmacol.129(7)1323-1332(2000) 2.McMahon, R.E., Marshall, F.J., and Culp, H.W.The nature of the metabolites of acetohexamide in the rat and in the humanJ. Pharmacol. Exp. Ther.149(2)272-279(1965) 3.Imamura, Y., Sanai, K., Seri, K., et al.Hypoglycemic effect of S(-)-hydroxyhexamide, a major metabolite of acetohexamide, and its enantiomer R(+)-hydroxyhexamideLife Sci.69(16)1947-1955(2001)