Design, synthesis and anxiolytic-like activity of 1-arylpyrrolo[1,2-a]pyrazine-3-carboxamides
| Autor: | G. V. Mokrov, O. A. Deeva, Yarkov Sa, T.A. Gudasheva, Yarkova Ma, S.B. Seredenin |
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| Rok vydání: | 2015 |
| Předmět: |
Male
Elevated plus maze Pyrazine Stereochemistry Clinical Biochemistry Pharmaceutical Science Gene Expression Anxiety Motor Activity Ligands Biochemistry Open field Anxiolytic like chemistry.chemical_compound Mice Structure-Activity Relationship Receptors GABA Drug Discovery Translocator protein medicine Animals Receptor Maze Learning Molecular Biology Mice Inbred BALB C Binding Sites Diazepam biology Dose-Response Relationship Drug Organic Chemistry Isoquinolines Amides chemistry Anti-Anxiety Agents Drug Design Pyrazines biology.protein Molecular Medicine Antagonism medicine.drug Protein Binding |
| Zdroj: | Bioorganicmedicinal chemistry. 23(13) |
| ISSN: | 1464-3391 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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