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Muzolimine is a small molecule, pyrazole-based high-ceiling loop diuretic that was used for the treatment of hypertension and kidney failure. It acts primarily by inhibiting sodium-potassium-chloride cotransporter (Na+K+Cl-) in the thick ascending limb of Henle’s loop, leading to increased excretion of sodium and water (diuresis). Muzolimine is considered to act as a prodrug; its active metabolite is secreted into the tubular lumen via a probenecid-sensitive pathway and inhibits Na+K+Cl- cotransport. The drug was withdrawn worldwide due to severe neurological side effects[1][3][4][5][6][7].
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