Bumetanide (sodium)

Bumetanide sodium, a highly potent loop diuretic, is a Na⁺-K⁺-Cl⁺ cotransporter (NKCC) blocker. Bumetanide sodium is a selective NKCC1 inhibitor, and also inhibits NKCC2, with IC₅₀s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively^[1][2]. In Vitro: Bumetanide sodium has inhibitory effects for the two major human splice variants of NKCCs, hNKCC1A and hNKCC2A ^[1].
Bumetanide sodium (0.03-100 μM; 5 minutes) inhibits the ⁸⁶Rb⁺ uptake in NKCC1A-expressing oocytes in a dose-dependent manner^[1].
Bumetanide sodium inhibits NKCC2 isoform B in HEK-293 cells with an IC₅₀ value of 0.54 μM^[2]. In Vivo: Bumetanide sodium (7.6-30.4 mg/kg; i.v.) attenuates the decrease in apparent diffusion coefficients (ADC) ratios for both cortex and striatum (by 40-67%), indicating reduced edema formation^[3].
Bumetanide sodium also reduces infarct size^[3].
Bumetanide sodium shows different half-lives of 21.4 min, 53.8 min and 137 min following 2 mg/kg, 8 mg/kg and 20 mg/kg intravenous injection, respectively, in rats^[4].