| Autor: |
Sa, Yarkov, Gv, Mokrov, Tatiana Gudasheva, Ma, Yarkova, Sb, Seredenin |
| Rok vydání: |
2016 |
| Předmět: |
|
| Zdroj: |
Europe PubMed Central |
| ISSN: |
0869-2092 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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