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Development and Study of Anxiolytic Effect of Gml-1 Tablet Dosage Form

  • M. A. YarkovaEmail author
  • E. V. Blynskaya
  • D. V. Yudina
  • G. V. Mokrov
  • T. A. Gudasheva
  • K. V. Alekseev
DRUG SYNTHESIS METHODS AND MANUFACTURING TECHNOLOGY
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Novel pyrrolo[1,2-a]pyrazine ligands of 18-kDa translocator protein (TSPO) were synthesized at Zakusov Research Institute of Pharmacology. Pharmacological studies of drug substance N-benzyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-1) were consistent with high affinity for TSPO and significant anxiolytic activity. A finished dosage form of GML-1 drug substance was developed and exhibited pronounced anxiolytic activity after intragastric administration over a wide dose range.

Keywords

pyrrolo[1,2-a]pyrazines finished dosage form 18-kDa translocator protein anxiolytic activity 

References

  1. 1.
    S. B. Seredenin, G. V. Mokrov, T. A. Gudasheva, et al., RU Pat. No. 2,572,076, Oct. 10, 2015.Google Scholar
  2. 2.
    S. A. Yarkov, G. V. Mokrov, T. A. Gudasheva, et al., Eksp. Klin. Farmakol., 79(1), 7 – 11 (2016).Google Scholar
  3. 3.
    P. M. Borodin, L. Shuler, and D. K. Belyaev, Genetika, 12(12), 62 – 71 (1976).Google Scholar
  4. 4.
    G. V. Mokrov, O. A. Deeva, T. A. Gudasheva, et al., Bioorg. Med. Chem., 23(13), 3368 – 3378 (2015).CrossRefGoogle Scholar
  5. 5.
    K. V. Alekseev, D. V. Yudina, E. V. Blynskaya, et al., Nauchn. Al’manakh, 12 – 2(26), 228 – 234 (2016).Google Scholar
  6. 6.
    R. G. Lister, Psychopharmacology, 92(1), 180 – 185 (1987).CrossRefGoogle Scholar
  7. 7.
    S. Pellow, P. Chopin, S. File, and M. Briley, J. Neurosci. Methods, 14, 149 – 167 (1985).CrossRefGoogle Scholar
  8. 8.
    S. V. Trofimov, E. F. Stepanova, and Yu. A. Obidchenko, Farmatsiya, 5, 33 – 36 (2015).Google Scholar
  9. 9.
    L. E. Gaevaya, L. N. Grushevskaya, M. S. Sergeeva, et al., Vestn. VolgGMU, 3(63), 29 – 32 (2017).Google Scholar

Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • M. A. Yarkova
    • 1
    Email author
  • E. V. Blynskaya
    • 1
  • D. V. Yudina
    • 1
  • G. V. Mokrov
    • 1
  • T. A. Gudasheva
    • 1
  • K. V. Alekseev
    • 1
  1. 1.V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical SciencesMoscowRussia

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