Amiloride HCl - CAS 2016-88-8
Catalog number: 2016-88-8
Category: Inhibitor
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Sodium Channel
Amiloride HCl is a relatively selective inhibitor of the epithelial sodium channel (ENaC), used in the management of hypertension and congestive heart failure.
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1.5'-Substituted amiloride derivatives as allosteric modulators binding in the sodium ion pocket of the adenosine A2A receptor.
Massink A, Louvel JA, Adlere I, van Veen C, Huisman BJ, Dijksteel GS, Guo D, Lenselink EB, Buckley BJ, Matthews H, Ranson M, Kelso MJ, IJzerman AP. J Med Chem. 2016 Apr 28. [Epub ahead of print]
The sodium ion site is an allosteric site conserved amongst many G protein-coupled receptors (GPCRs). Amiloride 1 and 5-(N,N-hexamethylene)amiloride 2 (HMA) supposedly bind in this sodium ion site and can influence orthosteric ligand binding. The availability of a high resolution X-ray crystal structure of the human adenosine A2A receptor (hA2AAR), in which the allosteric sodium ion site was elucidated, makes it an appropriate model receptor for investigating the allosteric site. In this study, we report the synthesis and evaluation of novel 5'-substituted amiloride derivatives as hA2AAR allosteric antagonists. Potency of the amiloride derivatives was assessed by their ability to displace the orthosteric radioligand [3H]4-(2-((7-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a]-[1,3,5]triazin-5-yl)amino)ethyl)phenol ([3H]ZM-241,385) from both the wild-type and sodium ion site W246A mutant hA2AAR. 4-Ethoxyphenethyl substituted amiloride 12l was found to be more potent than both amiloride and HMA, and the potency-shift between the wild-type and mutated receptor confirmed its likely binding to the sodium ion site.
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CAS 2016-88-8 Amiloride HCl

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