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The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities

The translocator protein (TSPO) promotes the translocation of cholesterol to the inner mitochondrial membrane and mediates steroid formation. In this study, we first report on a biological evaluation of the dipeptide GD-23 (N-carbobenzoxy-L tryptophanyl-L isoleucine amide), a structural analogue of...

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Autores principales: Povarnina, P. Yu., Yarkov, S. A., Gudasheva, T. A., Yarkova, M. A., Seredenin, S. B.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: A.I. Gordeyev 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4610171/
https://www.ncbi.nlm.nih.gov/pubmed/26483966
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author Povarnina, P. Yu.
Yarkov, S. A.
Gudasheva, T. A.
Yarkova, M. A.
Seredenin, S. B.
author_facet Povarnina, P. Yu.
Yarkov, S. A.
Gudasheva, T. A.
Yarkova, M. A.
Seredenin, S. B.
author_sort Povarnina, P. Yu.
collection PubMed
description The translocator protein (TSPO) promotes the translocation of cholesterol to the inner mitochondrial membrane and mediates steroid formation. In this study, we first report on a biological evaluation of the dipeptide GD-23 (N-carbobenzoxy-L tryptophanyl-L isoleucine amide), a structural analogue of Alpidem, the principal TSPO ligand. We show that GD-23 in a dose range of 0.05 to 0.5 mg/kg (i.p.) exhibits anxiolytic activity in the elevated plus maze test and nootropic activity in the object recognition test in scopolamine-induced amnesia in rodents. It was shown that GD-23 did not affect spontaneous locomotor activity, holding promise as a nonsedative anxiolytic agent. The anxiolytic and nootropic activities of GD-23 were abrogated by the TSPO specific ligand PK11195, which thus suggests a role for TSPO in mediating the pharmacological activity of GD-23.
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spelling pubmed-46101712015-10-19 The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities Povarnina, P. Yu. Yarkov, S. A. Gudasheva, T. A. Yarkova, M. A. Seredenin, S. B. Acta Naturae Research Article The translocator protein (TSPO) promotes the translocation of cholesterol to the inner mitochondrial membrane and mediates steroid formation. In this study, we first report on a biological evaluation of the dipeptide GD-23 (N-carbobenzoxy-L tryptophanyl-L isoleucine amide), a structural analogue of Alpidem, the principal TSPO ligand. We show that GD-23 in a dose range of 0.05 to 0.5 mg/kg (i.p.) exhibits anxiolytic activity in the elevated plus maze test and nootropic activity in the object recognition test in scopolamine-induced amnesia in rodents. It was shown that GD-23 did not affect spontaneous locomotor activity, holding promise as a nonsedative anxiolytic agent. The anxiolytic and nootropic activities of GD-23 were abrogated by the TSPO specific ligand PK11195, which thus suggests a role for TSPO in mediating the pharmacological activity of GD-23. A.I. Gordeyev 2015 /pmc/articles/PMC4610171/ /pubmed/26483966 Text en Copyright ® 2015 Park-media Ltd. http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Povarnina, P. Yu.
Yarkov, S. A.
Gudasheva, T. A.
Yarkova, M. A.
Seredenin, S. B.
The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities
title The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities
title_full The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities
title_fullStr The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities
title_full_unstemmed The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities
title_short The Novel Dipeptide Translocator Protein Ligand, Referred to As GD-23, Exerts Anxiolytic and Nootropic Activities
title_sort novel dipeptide translocator protein ligand, referred to as gd-23, exerts anxiolytic and nootropic activities
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4610171/
https://www.ncbi.nlm.nih.gov/pubmed/26483966
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