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

M. A. Yarkova; E. V. Blynskaya; D. V. Yudina; G. V. Mokrov; T. A. Gudasheva; K. V. Alekseev

doi:10.1007/s11094-019-02003-1

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

作者: Yarkova M.A.¹, Blynskaya E.V.¹, Yudina D.V.¹, Mokrov G.V.¹, Gudasheva T.A.¹, Alekseev K.V.¹
隶属关系:
1. V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences
期: 卷 53, 编号 4 (2019)
页面: 342-346
栏目: Drug Synthesis Methods and Manufacturing Technology
URL: https://ogarev-online.ru/0091-150X/article/view/245759
DOI: https://doi.org/10.1007/s11094-019-02003-1
ID: 245759

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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.