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Kovalev G.I.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | Kondrakhin E.A.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | Salimov R.M.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | Neznamov G.G.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology
Eksperimental'naya i Klinicheskaya Farmakologiya | Year: 2014

The effect of acute, 7-fold and 14-fold noopept (1 mg/kg/day) administration on the dynamics of anxiolitic and nootropic behavioral effects in cross-maze, as well as their correlations with NMDA- and BDZ-receptor density was studied in inbred mice strains, differing in exploratory and emotional status - C57BL/6 and BALB/c. The dipeptide failed to affect the anxiety and exploration activity in C57BL/6 mice at each of 3 steps of experimental session. In this strain the Bmax values of [3H]-MK-801 and [3H]-Flunitrazepam binding changed only after single administration. In respect to BALB/c mice noopept induced both the anxiolitic and nootropic effects reaching their maximum on 7th day. In BALB/c strain the dynamics of hippocampal NMDA-receptor binding corresponds to the dynamics of exploratory efficacy whereas the dynamics of BDZ-receptors in prefrontal cortex was reciprocally to dynamics of anxiety level. © Folium Publishing House, 2014. Source


Mokrov G.V.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | Deeva O.A.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | Gudasheva T.A.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | Yarkov S.A.,Federal State Budgetary Institution Research Zakusov Institute of Pharmacology | And 2 more authors.
Bioorganic and Medicinal Chemistry | Year: 2015

A series of 1-arylpyrrolo[1,2-. a]pyrazine-3-carboxamides were designed and synthesized as 18. kDa translocator protein (TSPO) ligands. Anxiolytic-like activity of compounds was evaluated in the open field test and elevated plus maze test. Compounds 1a and 1b demonstrated high anxiolytic-like effect in the dose range of 0.1-1.0. mg/kg comparable with that of diazepam. The involvement of TSPO receptor in the mechanism of anxiolytic-like activity of new compounds was proved by antagonism of the most active compound 1a with TSPO selective inhibitor PK11195. In vitro binding studies demonstrated high TSPO affinities for compounds 1a and 1b. © 2015 Elsevier Ltd. Source

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