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ЖУРНАЛЫ // Mendeleev Communications // Архив

Mendeleev Commun., 2024, том 34, выпуск 5, страницы 682–684 (Mi mendc219)

Communications

Tripeptide Phe-Trp-Leu-NH2 as a putative endogenous ligand of TSPO: molecular modeling, synthesis and pharmacological activity

O. A. Deevaa, A. S. Pantileeva, O. Yu. Kravtsovaa, S. V. Nikolaeva, N. A. Zefirovb, P. Yu. Povarninaa, T. A. Antipovaa, T. A. Gudashevaa, V. L. Dorofeeva

a Federal Research Center for Innovator and Emerging Biomedical and Pharmaceutical Technologies, Moscow, Russian Federation
b Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation


Аннотация: The putative endogenous tripeptide ligand of the translocator protein (TSPO) l-phenylalanyl-l-tryptophanyl-l-leucine amide was obtained using the drug-based peptide design strategy and molecular modeling. This tripeptide demonstrated anxiolytic activity in the elevated plus-maze test and antidepressant-like activity in the forced swimming test in BALB/c mice at the doses of 10 mg kg−1 (i.p.) and also showed neuroprotective activity in the concentration range of 10−5–10−7 m in vitro under conditions of oxidative stress using HT-22 neuronal cell line.

Ключевые слова: tripeptide, TSPO ligand, anxiolytic activity, antidepressant-like activity, neuroprotective activity.

Язык публикации: английский

DOI: 10.1016/j.mencom.2024.09.018



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