Bumetanide (Ro 10-6338;PF 1593) is a selective Na+-K+-Cl- cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[4].
References:
[1]. Frelin C, et al. Biochemical characterization of the Na+/K+/Cl- co-transport in chick cardiac cells. Biochem Biophys Res Commun. 1986 Jan 14;134(1):326-31.
[2]. Lykke K, 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. 2016 Jun;59:42-9.
[3]. Bourrit A, et al. Basic characterization of an ouabain-resistant, bumetanide-sensitive K+ carrier-mediated transport system in J774.2 mouse macrophage-like cell line and in variants deficient in adenylate cyclase and cAMP-dependent protein kinase activities. Biochim Biophys Acta. 1985 Jul 11;817(1):85-94.
[4]. Sandstr m PE. Evidence for diabetogenic action of bumetanide in mice. Eur J Pharmacol. 1988 May 20;150(1-2):35-41.