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Comparative Preclinical Pharmacokinetics and Bioavailability of Antidepressant GSB-106 Tablet Form
Bulletin of Experimental Biology and Medicine, 2019Pharmacokinetics and relative bioavailability of antidepressant GSB-106 (hexamethylendiamide bis-(N-monosuccinyl-L-seryl-L-lysine) were determined in rabbits after single oral administration of the pharmaceutical substance and tablet mass. GSB-106 concentrations in the blood plasma were determined by HPLC-mass spectrometry.
Victoria Bueva
exaly +3 more sources
Pharmaceutical Chemistry Journal, 2019
Studies at the V. V. Zakusov Science Research Institute of Pharmacology have worked on the basis of the β-pleated structure of loop 4 of brain-derived neurotrophic factor (BDNF) to construct its dimeric peptide mimetic - GSB-106, bis-(N-monosuccinyl-L-serine-L-lysine) hexamethylenediamide.
A. V. Tarasyuk +7 more
exaly +2 more sources
Studies at the V. V. Zakusov Science Research Institute of Pharmacology have worked on the basis of the β-pleated structure of loop 4 of brain-derived neurotrophic factor (BDNF) to construct its dimeric peptide mimetic - GSB-106, bis-(N-monosuccinyl-L-serine-L-lysine) hexamethylenediamide.
A. V. Tarasyuk +7 more
exaly +2 more sources
Bulletin of Experimental Biology and Medicine, 2013
Dimeric dipeptide GSB-106, a novel structural analogue of neurotrophin BDNF, in doses from 10(-5) to 10(-8) M protected cultured immortalized mouse hippocampal HT-22 neurons from H2O2 or glutamate damage. The neuroprotective effect of GSB-106 was also shown on cultured SH-SY5Y human neuroblastoma cells after treatment with neurotoxin 6-hydroxidopamine.
I O, Logvinov +5 more
exaly +3 more sources
Dimeric dipeptide GSB-106, a novel structural analogue of neurotrophin BDNF, in doses from 10(-5) to 10(-8) M protected cultured immortalized mouse hippocampal HT-22 neurons from H2O2 or glutamate damage. The neuroprotective effect of GSB-106 was also shown on cultured SH-SY5Y human neuroblastoma cells after treatment with neurotoxin 6-hydroxidopamine.
I O, Logvinov +5 more
exaly +3 more sources
Pharmaceutical Chemistry Journal, 2021
Antidepressant activities of the original compounds GSB-106 [bis(N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide], a mimetic of the fourth loop of brain-derived neurotrophic factor (BDNF); GML-3(N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide), a ligand of 18 kDa translocator protein (TSPO); and GZK-111 (N-phenylacetylglycyl-L ...
Anna Tallerova
exaly +2 more sources
Antidepressant activities of the original compounds GSB-106 [bis(N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide], a mimetic of the fourth loop of brain-derived neurotrophic factor (BDNF); GML-3(N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide), a ligand of 18 kDa translocator protein (TSPO); and GZK-111 (N-phenylacetylglycyl-L ...
Anna Tallerova
exaly +2 more sources
Synthesis of BDNF-mimetic dimeric dipeptide GSB-106, a potential neuroprotector drug
Pharmaceutical Chemistry Journal, 2013The BDNF-mimetic dimeric dipeptide bis-(N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide (GSB-106) based on the structure of beta-turn loop 4 (BDNF-Asp93-Ser94-Lys95-Lys96-) was synthesized. GSB-106 showed neuroprotective activity in vitro at concentrations 10–6-10–8 M and antidepressant activity in vivo in rats at i.p.
A. V. Tarasyuk +3 more
exaly +2 more sources
Russian Journal of Bioorganic Chemistry, 2014
In the previous work, we synthesized a dimeric dipeptide mimetic of the 4th loop of BDNF, i.e., hexamethylenediamide bis(N-monosuccinil-L-seryl-L-lysine) (GSB-106), which has neuroprotective activity in vitro in a concentration range of 10−5–10−8 M and antidepressant activity in vivo at intraperitoneal doses of 0.1 and 1 mg/kg in rats.
A. V. Tarasyuk +8 more
exaly +2 more sources
In the previous work, we synthesized a dimeric dipeptide mimetic of the 4th loop of BDNF, i.e., hexamethylenediamide bis(N-monosuccinil-L-seryl-L-lysine) (GSB-106), which has neuroprotective activity in vitro in a concentration range of 10−5–10−8 M and antidepressant activity in vivo at intraperitoneal doses of 0.1 and 1 mg/kg in rats.
A. V. Tarasyuk +8 more
exaly +2 more sources
Low-Molecular-Weight Compound GSB-106 Mimics the Cellular Effects of BDNF after Serum Deprivation
Doklady Biochemistry and Biophysics, 2019The in vitro model of serum deprivation shows that the survival of SH-SY5Y neuronal cells is ensured by the intrinsic trophic activity of BDNF loop 4-th mimetic GSB‑106 (10-7 М), which is comparable to that of endogenous neurotrophin (10-9 М). The analysis of the cell cycle and S‑phase showed that GSB‑106, like BDNF, induces cell cycle arrest in the G1
L F, Zainullina +3 more
openaire +2 more sources