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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]


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.

[PubMed - indexed for MEDLINE]
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