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SYNTHESIS OF THE PHARMACOLOGICALLY ACTIVE ANALOG OF THE GSB-106, DIPEPTID MIMETIC OF BDNF
DOI: https://doi.org/10.29296/25877313-2019-07-01
Issue:
7
Year:
2019
Previously the dimeric dipeptide mimetic bis-(N-monosuccinil-L-seryl-L-lysine) hexamethylenediamide (GSB-106) was created in Zakusov Institute of Pharmacology. GSB-106 demonstrates neuroprotective activity in vitro under oxidative stress conditions in concentrations of 10–5–10–7 M and also it demonstrates antidepressant activity in behavioral tests in rodents i.p. in the doses of 0.1–1.0 mg/kg. The acetyl analog of GSB-106, bis-(N-acetyl-L-seryl-L-lysine) hexamethylenediamide (GTS-106Ac), was synthesized to study the role of the N-acyl radical in the activity of the GSB-106. The study of the neuroprotective activity of GTS-106Ac on the neuronal HT-22 culture under conditions of oxidative stress showed this activity in concentrations of 10–5–10–8 M. In the test of Porsolt in mice, i.p., GTS-106Ac showed the antidepressant effect in the doses of 1.0 and 5.0 mg/kg, significantly reducing the time of immobility of the animals compared with control group of animals.
Keywords:
BDNF
mimetic
dipeptide
GSB-106
GTS-106Ac
neuroprotective activity
antidepressant activity
peptide synthesis
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