Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

uPA:7 μM(Ki)

In salt-sensitive hypertensive animals, Amiloride antagonizes or blocks the action of aldosterone in cells, as well as within vascular and renal tissues. Daily subcutaneous injections of 1 mg/kg Amiloride in DOCA-salt hypertensive rats reversed the initial increase in collagen deposition. In stroke-prone spontaneously hypertensive rats, Amiloride administration via saline drinking water delayed the onset of proteinuria and improved histological scores in brain and kidney tissues compared to controls.

Upon increased perfusion pressure, 1 μM Amiloride and 30 nM Benzamil inhibit myogenic responses by blocking the activity of ENaC proteins, thereby suppressing vasoconstriction. In vascular smooth muscle cells, Amiloride completely inhibits sodium influx. Amiloride is a relatively selective inhibitor of epithelial sodium channels (ENaC) with an IC 50 of 0.1 μM to 0.5 μM. Although less effective as a Na+/H+ exchanger (NHE) inhibitor, Amiloride's IC 50 values range from as low as 3 μM at low external sodium concentrations to 1 mM at high external sodium concentrations. Furthermore, Amiloride exerts a weak inhibitory effect on Na+/Ca2+ exchange (NCX) with an IC 50 of 1 mM.