Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 13, Pages 3368-3378Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.04.049
Keywords
Anxiolytic activity; Elevated plus maze test; Open field test; PK11195; Pyrrolo[1,2-a]pyrazines; TSPO; Vinyl azides
Funding
- Basic Research Program of the Presidium of the Russian Academy of Sciences
Ask authors/readers for more resources
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. (C) 2015 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available