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Fiziologichnyi Zhurnal - <a id="lj1_ret_bk_to_jl0_href_id" href="?list0=13">Fiziol. Zh. 2011;</a> <a id="lj1_ret_bk_to_jl0_href_id" href="?list1=67">57(6):</a> 31-37
Українська Русский English

ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)
DOI: https://doi.org/10.15407/fz

Fiziologichnyi Zhurnal

is a scientific journal issued by the

Bogomoletz Institute of Physiology
National Academy of Sciences of Ukraine

Editor-in-chief: V.F. Sagach

The journal was founded in 1955 as
1955 – 1977 "Fiziolohichnyi zhurnal" (ISSN 0015 – 3311)
1978 – 1993 "Fiziologicheskii zhurnal" (ISSN 0201 – 8489)
1994 – 2016 "Fiziolohichnyi zhurnal" (ISSN 0201 – 8489)
2017 – "Fiziolohichnyi zhurnal" (ISSN 2522-9028)

Fiziol. Zh. 2011; 57(6): 31-37

(3-carboxamidino-2-oxo-2h-chromen-7-yl)-4-guanidinobenzoates are novel blockers of acidsensing ion channels

V. A. Sukach, A.Z. Buta, O.P. Maximyuk, D.B. Kovalskyy, M.V. Vovk, O.O. Krishtal.

    Ін-т органічної хімії НАН України, Київ;Ін-т фізіології ім. О.О.Богомольця НАН України, Київ;Міжнар. центр молекул. фізіології НАН України, Київ


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 uM. Our data suggest that 3-carboxamidinocoumarines can be used as a scaffold for novel type of highly efficient anti-ischemic drugs.

Keywords: 3-амидино-7-гидроксикумарины,блокаторы рН-чувствительных ионных каналов, антиише-мические препараты.


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