| Literature DB >> 2852509 |
C Frelin1, P Barbry, P Vigne, O Chassande, E J Cragoe, M Lazdunski.
Abstract
Amiloride analogs inhibit a number of transmembrane Na+ transport systems: 1) the epithelium Na+ channel, 2) the Na+/H+ exchange system and 3) the Na+/Ca2+ exchange system. Structure--activity relationships using amiloride derivatives with selected modification of each of the functional groups of the molecule indicate that the 3 Na+ transporting systems have distinct pharmacological profiles. 5-N Disubstituted derivatives of amiloride, such as ethylisopropylamiloride are the most potent inhibitors of the Na+/H+ exchange system. Conversely, amiloride derivatives that are substituted on the guanidino moiety, such as phenamil, are potent inhibitors of the epithelium Na+ channel. It is thus possible, by using selected amiloride derivatives to inhibit selectively one or another of the Na+ transport systems.Entities:
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Year: 1988 PMID： 2852509 DOI： 10.1016/0300-9084(88)90196-4
Source DB: PubMed Journal: Biochimie ISSN： 0300-9084 Impact factor: 4.079