Open AccessThe novel dipeptide ligand of TASP
Author(s) -
O. A. Deeva,
O. A. Deeva,
А. S. Pantileev,
Андрей Сергеевич Пантилеев,
I. V. Rybina,
I. V. Rybina,
М. А. Yarkova,
М. А. Yarkova,
Т. А. Gudasheva,
Т. А. Гудашева,
С. Б. Середенин,
С. Б. Середенин
Publication year - 2019
Publication title -
doklady akademii nauk. rossijskaâ akademiâ nauk
Language(s) - English
Resource type - Journals
ISSN - 0869-5652
DOI - 10.31857/s0869-56524842228-232
Subject(s) - dipeptide , chemistry , anxiolytic , antagonist , amide , ligand (biochemistry) , stereochemistry , open field , pharmacology , peptide , receptor , biochemistry , medicine
Using the previously obtained first dipeptide ligand TSPO the N‑carbobenzoxy-L‑tryptophanyl-L‑isoleucine amide (GD‑23) as a basis, the new dipeptide was synthesized — the N‑phenylpropionyl–L‑tryptophanyl-L‑leucine amide (GD‑102). GD‑102 expressed anxiolytic activity in the open field test in BALB/c mice and in the elevated plus maze test in ICR mice. The minimum effective dose of GD‑102 was an order of magnitude lower than that of GD‑23. Preliminary administration of the TSPO selective antagonist, compound PK11195, completely blocked the anxiolytic activity of GD‑102, that indicated the participation of TSPO in the realization of the anxiolytic action GD‑102. The results were confirmed by molecular docking data.