Email this article Novel Pyrrolo[1,2-a]Pyrazines (TSPO Ligands) with Anxiolytic Activity Dependent on Neurosteroid Biosynthesis
- Authors: Yarkova M.A.1, Mokrov G.V.1, Gudasheva T.A.1, Seredenin S.B.1
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Affiliations:
- Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
- Issue: Vol 50, No 8 (2016)
- Pages: 501-504
- Section: Molecular-Biological Problems of Drug Design and Mechanism of Drug Action
- URL: https://journals.rcsi.science/0091-150X/article/view/244423
- DOI: https://doi.org/10.1007/s11094-016-1476-0
- ID: 244423
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Abstract
A series of novel pyrrolo[1,2-a]pyrazines that were ligands of 18 kDa translocator protein (TSPO) were synthesized at Zakusov SIP. The compounds N-benzyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-1) and N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) were found to possess high TSPO affinity and pronounced anxiolytic activity. The anxiolytic effects of GML-1 and GML-3 in elevated plus-maze tests were completely blocked by the neurosteroidogenic-enzyme inhibitors trilostane and finasteride.
About the authors
M. A. Yarkova
Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Author for correspondence.
Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
G. V. Mokrov
Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
T. A. Gudasheva
Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
S. B. Seredenin
Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences
Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
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