The First Dipeptide Mimetic of Neurotrofin-3: Design and Pharmacological Properties.

Autor: Gudasheva TA; Zakusov Research Institute of Pharmacology, Moscow, Russia. tata-sosnovka@mail.ru., Sazonova NM; Zakusov Research Institute of Pharmacology, Moscow, Russia., Tarasiuk AV; Zakusov Research Institute of Pharmacology, Moscow, Russia., Logvinov IO; Zakusov Research Institute of Pharmacology, Moscow, Russia., Antipova TA; Zakusov Research Institute of Pharmacology, Moscow, Russia., Nikiforov DM; Zakusov Research Institute of Pharmacology, Moscow, Russia., Povarnina PY; Zakusov Research Institute of Pharmacology, Moscow, Russia., Seredenin SB; Zakusov Research Institute of Pharmacology, Moscow, Russia.
Jazyk: angličtina
Zdroj: Doklady. Biochemistry and biophysics [Dokl Biochem Biophys] 2022 Aug; Vol. 505 (1), pp. 160-165. Date of Electronic Publication: 2022 Aug 29.
DOI: 10.1134/S1607672922040032
Abstrakt: The dimeric dipeptide mimetic hexamethylenediamide bis-(N-monosuccinyl-L-asparaginyl-L-asparagine) (GTS-301) was created on the basis of the structure of the exposed region of the neurotrophin-3 4th loop. The new compound, as well as the full-length neurotrophin, activated the TrkC and TrkB receptors. GTS-301 showed neuroprotective activity in experiments on HT-22 mouse hippocampal cells under conditions of oxidative stress and glutamate toxicity at concentrations of 10 -12 and 10 -8 M, respectively, and antidepressant-like activity in the forced swimming test on mice with 7-day intraperitoneal administration in doses of 10-40 mg/kg.
(© 2022. Pleiades Publishing, Ltd.)
Databáze: MEDLINE
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