Mechanism of action of amiloride: a molecular prospective
Kleyman, T.R.; Sheng, S.; Kosari, F.; Kieber-Emmons, T.
Seminars in Nephrology 19(6): 524-532
1999
ISSN/ISBN: 0270-9295 PMID: 10598540 Document Number: 510863
Amiloride is a prototypic inhibitor of epithelial sodium channels. Rapid progress has been made in our understanding of the structure of the sodium channel and related cation-selective channels. This work, coupled with experiments examining how selected sodium channel mutations affect amiloride binding, provides critical clues towards defining sites within the channel that bind amiloride. Residues within the channel pore and within its extracellular domain participate in amiloride binding. These results suggest that sites that interact with amiloride within the channel's extracellular domain may be in close proximity to residues within the channel's pore.