N-Phenylacetylglycyl-L-Proline Ethyl Ester Converts into Cyclo-L-Prolylglycine Showing a Similar Spectrum of Neuropsychotropic Activity
- Authors: Gudasheva T.A.1, Kolyasnikova K.N.1, Kuznetsova E.A.1, Litvinova S.A.1, Zolotov N.N.1, Voronina T.A.1, Ostrovskaya R.U.1, Seredenin S.B.1
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Affiliations:
- V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
- Issue: Vol 50, No 11 (2017)
- Pages: 705-710
- Section: Search for New Drugs
- URL: https://journals.rcsi.science/0091-150X/article/view/244463
- DOI: https://doi.org/10.1007/s11094-017-1516-4
- ID: 244463
Cite item
Abstract
Previously designed cyclo-L-prolylglycine (CPG), a peptide prototype of piracetam, was discovered as an endogenous compound in rat brain and exhibited nootropic and anxiolytic properties. N-Phenylacetylglycyl-L-proline ethyl ester (GZK-111) was synthesized in the present work. It was established that GZK-111 converted to CPG and possessed nootropic, anxiolytic, and antihypoxic activities typical of CPG at doses of 0.1 – 1.5 mg/kg (i.p.). The effects of both GZK-111 and CPG were stereoselective with only the L-enantiomers being active. GZK-111 could be considered as a prodrug that enhanced cognitive functioning with an anxiolytic component.
About the authors
T. A. Gudasheva
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
K. N. Kolyasnikova
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
E. A. Kuznetsova
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
S. A. Litvinova
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
N. N. Zolotov
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
T. A. Voronina
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
R. U. Ostrovskaya
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315
S. B. Seredenin
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
Russian Federation, 8 Baltiiskaya St., Moscow, 125315