A first generation sulfonylurea
Carbutamide is a first generation sulfonylurea.1 It inhibits ATP-sensitive potassium (KATP) channels in β-cells with an IC50 value of 173 ?M.2 It reduces blood glucose levels in anesthetized dogs when administered at a dose of 50 mg/kg.3 Carbutamide also increases ventricular fibrillation in a rat model of cardiac ischemia induced by left anterior descending (LAD) coronary artery ligation.1 Formulations containing carbutamide have previously been used in the treatment of diabetes.
1.Ballagi-Pordány, G., K?szeghy, A., Koltai, M.Z., et al.Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compoundsDiabetes Res. Clin. Pract.8(2)109-114(1990) 2.Schwanstecher, C., Meyer, M., Schwanstecher, M., et al.Interaction of N-benzoyl-D-phenylalanine and related compounds with the sulphonylurea receptor of β-cellsBr. J. Pharmacol.123(6)1023-1030(1998) 3.Pozza, G., Galansino, G., and Foà, P.P.Insulin secretion following carbutamide injections in normal dogsProc. Soc. Exp. Biol. Med.93(3)539-542(1956)
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