Description
Bumetanideisaloopdiureticthatisclinicallyusedtotreatcongestiveheartfailure.Bumetanideexhibitsnatriureticactivity,inhibitingNa+/K+/2Cl-symporter1(NKCC1)andK+/Ca2+co-transporter2(KCC2),decreasingfluidsecretionandNa+/K+transport.Bumetanidealsoexhibitsanxiolytic,neuroprotective,andantiepileptic/anticonvulsantactivities.Bumetanideinduceshyperpolarizationinkidneycells,increasingwhole-cellconductanceandintracellularCa2+levels.Inanimalmodels,bumetanidedecreasesconditionedanxietyincontextualfearandstartleassays.Ininjuredneurons,thiscompoundinhibitsupregulationoflow-affinityNGF/pan-neurotrophinreceptorp75NTR,preventingcelldeath.Additionally,bumetanide’sinhibitionofNKCC1co-transportersinneuronsaltersGABAsignaling,inhibitingseizure-inducedaccumulationofCl-andfacilitationofrecurrentseizuresinvivo.
References
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