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


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Abstract

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.

About the authors

M. A. Yarkova

V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences

Author for correspondence.
Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315

E. V. Blynskaya

V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences

Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315

D. V. Yudina

V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences

Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315

G. V. Mokrov

V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences

Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315

T. A. Gudasheva

V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences

Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315

K. V. Alekseev

V. V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences

Email: doctorpharm@mail.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315

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