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Fiziol Zh. 2011;57(6):31-7.

[(3-carboxamidino-2-oxo-2H-chromen-7-yl)-4-guanidinobenzoates are novel blockers of pH-sensitive ion channels].

[Article in Ukrainian]

Abstract

Ischemic stroke is one of the most severe brain pathologies that is extremely difficult to treat. Recently it has been found that acidosis accompanying cerebral ischemia induces activation of acid-sensing ion channel ASIC1a which results in its turn in the neuronal death. Here we present novel derivatives of 3-carboxamidinocoumarines that effectively inhibit ASIC1a and ASIC3 channels in concentration-dependent manner. The most active compound inhibits ASIC1a and ASIC3 channels with corresponding IC50 of 7.3 and 13.2 microM. Our data suggest that 3-carboxamidinocoumarines can be used as a scaffold for novel type of highly efficient anti-ischemic drugs.

PMID:
22420156
[PubMed - indexed for MEDLINE]
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