Title |
[PHARMACOLOGICAL STUDY OF NEW COMPOUNDS ACTING AS REGULATORS OF 18-KDA TRANSLOCATOR PROTEIN LIGANDS].
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Published in |
Eksperimental naia i klinicheskaia farmakologiia, January 2016
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DOI | 10.30906/0869-2092-2016-79-1-7-11 |
Pubmed ID | |
Authors |
Станислав Алексеевич Ярков, Григорий Владимирович Мокров, Татьяна Алексеевна Гудашева, Милада Арнольдовна Яркова, Сергей Борисович Середенин |
Abstract |
The interaction of new original 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamide derivatives with mitochondrial translocator protein (MTP) 18 kDa has been studied by radioligand binding assay. Compounds GML-1 (Ki = 5.2 x 10⁻⁸ M) and GML-3 (Ki = 5.3 x 10⁻⁷ M) exhibit high binding affinity for MTP. GML-1 and GML-3 in a dose range of 0.1-1 mg/kg (i.p.) demonstrated anxiolytic-like effects in the elevated plus-maze test in CD-1 mice, which were blocked by the MTP selective antagonist PK11195. The data obtained on the molecular target, anxiolytic-like effects and low toxicity GML-1 and GML-3 suggest that these compounds are promising for further investigation as anxiolytics. |
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