Synthesis and Biological Properties of a New Dipeptide Mimetic of Brain-Derived Neurotrophic Factor Loop 2**.

Autor:	Sazonova, N. M., Tarasyuk, A. V., Shumskii, A. N., Povarnina, P. Yu., Kruglov, S. V., Antipova, T. A., Gudasheva, T. A., Seredenin, S. B.
Předmět:	DIPEPTIDES OXIDATIVE stress ANTIOXIDANTS GABA agonists ENZYMES
Zdroj:	Pharmaceutical Chemistry Journal; Dec2018, Vol. 52 Issue 9, p763-770, 8p
Abstrakt:	A dimeric dipeptide mimetic of brain-derived neurotrophic factor loop 2, bis-(N-hexanoyl-seryl-lysine) hexamethylenediamide or GTS-201, was designed and synthesized. It exhibited neuroprotective activity at concentrations of 10-5 - 10-8 M in HT-22 immortalized hippocampal neuronal cell culture under H2O2-induced oxidative stress. Western-blot analysis showed that it activated TrkB receptors and Erk but not Akt. GTS-201 did not exhibit antidepressant activity in a Porsolt forced swim test on BALB/c mice at i.p. doses of 0.1, 1.0, and 5.0 mg/kg, in contrast with previously synthesized GSB-106, a dimeric dipeptide mimetic of loop 4. The results confirmed the previous original hypothesis about the possible discrimination of neurotrophin functions by low-molecular-mass mimetics of their separate loops. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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