Bumetanide-d5 is intended for use as an internal standard for the quantification of bumetanide by GC- or LC-MS. Bumetanide is a loop diuretic with good absorption and pharmacodynamic properties.1,2 It acts as an inhibitor of the Na-K-Cl cotransporter 1 (NKCC1) and the kidney-specific NKCC2 (Kis = 0.5 and 59 μM for human and rabbit NKCC1, respectively).3,4 Bumetanide also inhibits several isoforms of carbonic anhydrase.5
1.Ramsay, L.E., McInnes, G.T., Hettiarachchi, J., et al.Bumetanide and frusemide: A comparison of dose-response curves in healthy menBr. J. Clin. Pharmacol.5(3)243-247(1978) 2.Marcantonio, L.A., Auld, W.H.R., Murdoch, W.R., et al.The pharmacokinetics and pharmacodynamics of the diuretic bumetanide in hepatic and renal diseaseBr. J. Clin. Pharmacol.15(2)245-252(1983) 3.Horster, M.Embryonic epithelial membrane transportersAm. J. Physiol. Renal Physiol.279(6)982-996(2000) 4.Gillen, C.M., Brill, S., Payne, J.A., et al.Molecular cloning and functional expression of the K-Cl cotransporter from rabbit, rat, and human. A new member of the cation-chloride cotransporter familyJ. Biol. Chem.271(27)16237-16244(1996) 5.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 adductBioorg. Med. Chem. Lett.18(8)2567-2573(2008)