Publications on the project |
106 Novel Derivatives of Coumarin-3-Carboxamidines Inhibit Acid-Sensing Ion Channels (ASICs) in Low Micromolar Concentrations |
Authors: | V. A. Sukach, A. Z. Buta, O. P. Maximyuk, D. B. Kovalskyy, M. V. Vovk, O. O. Krishtal | |
Summary: | Ischemic stroke is one of the most severe brain pathologies, which 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 coumarin-3-carboxamidines 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 µM. Our data suggest that coumarin-3-carboxamidino can be used as a scaffold for novel type of highly efficient anti-ischemic drugs. | |
Keywords: | coumarin-3-carboxamidines , ASICs blockers, anti-ischemic drugs | |
Edition: | International Journal of Physiology and Pathophysiology | | | 2012,
,English |
The events in the framework of the project |
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106 6. Nanochemistry Purpose: Expected results:Release of new product: material Stage 1: Stage 2: Stage 3: Stage 4: Stage 5:
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