Design and synthesis of a novel dipeptide mimetic of the 4th loop of neurotrophin-3 and its pharmacological effects

被引：1

作者：

Tarasiuk, Alexey, V ^{[1
]}

Sazonova, Nellya M. ^{[1
]}

V. Melnikova, Marina ^{[1
]}

V. Pomogaybo, Sergey ^{[1
]}

Logvinov, Ilya O. ^{[1
]}

Nikolaev, Sergey, V ^{[1
]}

Nikiforov, Dmitry M. ^{[1
]}

Antipova, Tatiana A. ^{[1
]}

Povarnina, Polina Yu. ^{[1
]}

Vakhitova, Yulia V. ^{[1
]}

Gudasheva, Tatiana A. ^{[1
]}

Seredenin, Sergey B. ^{[1
]}

机构：

[1] VV Zakusov Res Inst Pharmacol, Moscow 125315, Russia

来源：

MENDELEEV COMMUNICATIONS | 2023年 / 33卷 / 06期

关键词：

dipeptide mimetic; low-molecular mimetic; design; neurotrophin-3; cytoprotective activity; antidepressant-like activity; TRKA;

D O I：

10.1016/j.mencom.2023.10.016

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A novel neurotrophin-3 loop 4 dipeptide mimetic, bis(N-y-hydroxybutyryl-l-glutamyl-l-asparagine) hexamethylenedi-amide (GTS-302), was designed and synthesized. Compound GTS-302 activated the tyrosine kinase receptors TrkC and TrkB, exhibited cytoprotective activity (10-8-10-5 M) in oxidative stress model in HT-22 cells and in 6-hydroxy-dopamine-induced SH-SY5Y cell damage. It also demon-strated an antidepressant-like activity in the forced swim test in mice (0.5-10.0 mg kg-1, intraperitoneally).

引用

页码：786 / 789

页数：4

共 36 条

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