Amiloride is a reversible inhibitor of acid-sensing ion channels (ASICs) and epithelial sodium channels (ENaCs), with a reported IC₅₀ value of approximately 10 µM for blocking ASIC1a currents. It exhibits potent activity in reducing neuronal firing and contractile responses, with a rank order of potency for ASIC1a inhibition being benzamil > phenamil > DMA > amiloride. In research, it is widely used to study neuroinflammation, ion channel physiology, and erectile function, often at concentrations ranging from 10 to 100 µM in vitro. Amiloride also serves as a scaffold for developing more selective analogs targeting ASIC subtypes and fungal pathogens.