Mechanism of action of amiloride: a molecular prospective.
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.
Kleyman
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TR
Department of Medicine, University of Pennsylvania and VA Medical Center, Philadelphia, USA.
Sheng
S
S
Kosari
F
F
Kieber-Emmons
T
T
D000584:Amiloride / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001692:Biological Transport / Q000187:drug effects / Q000502:physiology; D004232:Diuretics / Q000737:chemistry / Q000494:pharmacology*; D004848:Epithelium / Q000187:drug effects / Q000378:metabolism; D007668:Kidney / Q000187:drug effects / Q000502:physiology; D008967:Molecular Biology; D012680:Sensitivity and Specificity; D015222:Sodium Channels / Q000187:drug effects* / Q000502:physiology
D004232:Diuretics; D015222:Sodium Channels; D000584:Amiloride