Bumetanide

Bumetanide is an inhibitor of Na-K-2Cl cotransporter 1 (NKCC1; IC₅₀ = 0.68 µM).¹ It is selective for NKCC1 over NKCC2 (IC₅₀ = 4 µM). Bumetanide is an agonist of G protein-coupled receptor 35 (GPR35; EC₅₀ = 10 µM).² It also inhibits various carbonic anhydrases.³ Bumetanide (0.1 mg/kg) increases urine flow and sodium and potassium excretion, as well as decreases sodium reabsorption, in anesthetized dogs.⁴ It reduces brain edema and infarct size in a rat model of stroke induced by permanent middle cerebral artery occlusion (MCAO) when administered at doses ranging from 7.6 to 30.4 mg/kg.⁵ Formulations containing bumetanide have been used in the treatment of edema associated with congestive heart failure and hepatic and renal diseases.

WARNING This product is not for human or veterinary use.

1. Lykke, K., Töllner, K., Feit, P.W., et al. The search for NKCC1-selective drugs for the treatment of epilepsy: Structure-function relationship of bumetanide and various bumetanide derivatives in inhibiting the human cation-chloride cotransporter NKCC1A. Epilepsy Behav. 59, 42-49 (2016).

2. Yang, Y., Fu, A., Wu, X., et al. GPR35 is a target of the loop diuretic drugs bumetanide and furosemide. Pharmacology 89(1-2), 13-17 (2012).

3. Temperini, C., Cecchi, A., Scozzafava, A., et al. Carbonic anhydrase inhibitors. Interaction of indapamide and related diuretics with 12 mammalian isozymes and X-ray crystallographic studies for the indapamide-isozyme II adduct. Bioorg. Med. Chem. Lett. 18(8), 2567-2573 (2008).

4. Cohen, M.R., Hinsch, E., Vergona, R., et al. A comparative diuretic and tissue distribution study of bumetanide and furosemide in the dog. J. Pharmacol. Exp. Ther. 197(3), 697-702 (1976).

5. O'Donnell, M.E., Tran, L., Lam, T.I., et al. Bumetanide inhibition of the blood-brain barrier Na^-K^-Cl cotransporter reduces edema formation in the rat middle cerebral artery occlusion model of stroke. J. Cereb. Blood Flow Metab. 24(9), 1046-1056 (2004).