| Literature DB >> 3396627 |
J Velly1, M Grima, N Decker, E J Cragoe, J Schwartz.
Abstract
The ability of amiloride and its analogues to inhibit [3H]batrachotoxinin-A 20-alpha benzoate [( 3H]BTX-B) and [3H]tetracaine binding to rat synaptosomes and to a rat heart membrane preparation was tested. Their ability to inhibit 22Na influx was determined with rat synaptosomes. 5-N-substituted analogues were generally more potent in inhibiting [3H]BTX-B and [3H]tetracaine binding than compounds substituted on the guanidine group. However, the inhibition was not competitive. Amiloride and some of its analogues were as active or more active in inhibiting [3H]tetracaine binding than they were in inhibiting [3H]BTX-B binding. 22Na influx was inhibited with the same relative potencies as [3H]BTX-B binding and a good correlation was found between the two inhibitions. These results show an effect of amiloride and its analogues on the voltage-sensitive Na+ channels, which could partly explain the inotropic effects of these drugs.Entities:
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Year: 1988 PMID： 3396627 DOI： 10.1016/0014-2999(88)90047-7
Source DB: PubMed Journal: Eur J Pharmacol ISSN： 0014-2999 Impact factor: 4.432