A5004610189- Biochemical effects in animals
- Neuroscience and Neuropharmacology Research
- Nerve injury and regeneration
- Neuropeptides and Animal Physiology
- Pharmacological Receptor Mechanisms and Effects
- Tryptophan and brain disorders
- Neurological Disorders and Treatments
- Stress Responses and Cortisol
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Neurotransmitter Receptor Influence on Behavior
- Neurogenesis and neuroplasticity mechanisms
- Cholinesterase and Neurodegenerative Diseases
- Carcinogens and Genotoxicity Assessment
- Axon Guidance and Neuronal Signaling
- Synthesis and biological activity
- Eicosanoids and Hypertension Pharmacology
- Chemical Reactions and Isotopes
- Neuroendocrine regulation and behavior
- Neurological Disease Mechanisms and Treatments
- Pharmacological Effects of Natural Compounds
- Cancer therapeutics and mechanisms
- RNA Interference and Gene Delivery
- Adipose Tissue and Metabolism
- Amino Acid Enzymes and Metabolism
Federal Medical-Biological Agency
2025
Institute of Pharmacology Russian Academy of Medical Sciences
2015-2024
Institute of Pharmacology
1999-2020
Academy of the Federal Security Service of the Russian Federation
2018
Pirogov Russian National Research Medical University
1989-2016
Academy of Medical Sciences
1997-2015
Russian Academy of Sciences
2001-2015
University of South Florida
2013
Florida College
2013
Genetika
2013
Background: Two dimeric dipeptides, bis -(N-monosuccinyl-L-seryl-L-lysine)hexamethylenediamide (GSB-106) and -(N-monosuccinyl-L-methionyl-L-serine) heptamethylenediamide (GSB-214), were designed based on the brain-derived neurotrophic factor (BDNF) loop 4 1 β-turn sequences, respectively. Earlier, both of these dipeptides shown to exhibit neuroprotective activity in vitro (10 -5 –10 -8 M). The present study aimed investigate mechanisms action peptides their an experimental stroke model....
This study aimed at developing nerve growth factor (NGF) mimetics that selectively activate specific biological signals and, as a result, lack the side effects of full-length protein. Two dimeric dipeptides, bis-(N-aminocaproyl-glycyl-L-lysine) hexamethylenediamide (GK-6) and bis(N-succinyl-L-glutamyl-L-lysine) (GK-2), were designed based on most exposed outside fragments NGF, namely, loop 1 4 β-turn sequences, respectively. These dipeptides exhibited neuroprotective activity in vitro...
Using high‐performance liquid chromatography, gas‐chromatography and chromato‐mass spectrometry methods a novel endogenous cyclic dipeptide cyclo‐prolylglycine was identified in rat brain. Its content according to gas chromatography is 2.8 ± 0.3 nmol/g wet Synthetic has demonstrated antiamnesic activity the passive avoidance test rats at dose of 0.1 mg/kg i.p. Cyclic seems be memory facilitating substance its presence brain suggests existence new mechanism regulation.
Alzheimer's disease (AD) is a progressive neurodegenerative and the leading cause of senile dementia in United States. Accumulation amyloid-<i>β</i> (A<i>β</i>) effects this peptide on microglial cells contribute greatly to etiology AD. Experiments were carried out determine whether pan-selective <i>σ</i>-receptor agonist afobazole can modulate response cytotoxic A<i>β</i> fragment, A<i>β</i><sub>25–35</sub>. Treatment with decreased activation A<i>β</i>, as indicated by reduced membrane...
Thirteen behavioral variables from six tasks were measured in alcohol‐preferring (AA, FH, and P) ‐non‐preferring (ANA, FRL, NP) rat lines/strains subjected to Factor Analysis. Four independent factors accounted for >90% of the variance. Defecation open field ultrasonic vocalizations after an air puff negatively correlated with alcohol intake preference, whereas increase daily fluid presence saccharin was positively correlated. Other could be labeled Activity, Emotionality, Immobility...
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by continual decline of cognitive function. No therapy has been identified that can effectively halt or reverse its progression. One hallmark AD accumulation the amyloid-<i>β</i> peptide (A<i>β</i>), which alone induces neuronal injury via various mechanisms. Data presented here demonstrate prolonged exposure (1–24 hours) rat cortical neurons to A<i>β</i><sub>25–35</sub> results in an increase basal intracellular...
A mimetic of the BDNF loop 4, bis (N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide, named GSB-106, was designed and synthesized in our scientific group. The compound activated TrkB, MAPK/ERK, PI3K/AKT, PLCγ vitro experiments. In vivo experiments with rodents revealed its antidepressant-like activity forced swim tail suspension tests at dose range 0.1–5.0 mg/kg (i.p., p.o.). However, GSB-106 not studied depression models modulating major humans. present study, mice model induced by...
Background: A dipeptide mimetic of the BDNF loop 4, bis (N-monosuccinyl-L-seryl-L-lysine) hexamethylenediamide, GSB-106, was designed and synthesized by V.V. Zakusov Research Institute Pharmacology. The compound activated in vitro TrkB, MAPK/ERK, PI3K/AKT, PLCγ, like full-length BDNF. In vivo, GSB-106 exhibited antidepressant-like, neuroprotective neuroregenerative properties. aim this work to study effects on depressive-like behavior, cognitive impairments, as well hippocampal...
Abstract The neuroprotective activity of a novel N ‐acylprolyl‐containing dipeptide analog the nootropic 2‐oxo‐1‐pyrrolidine acetamide (Piracetam) designated as GVS‐111 (DVD‐111/Noopept) was tested in two vitro models neuronal degeneration mediated by oxidative stress: normal human cortical neurons treated with H 2 O , and Down's syndrome (DS) neurons. Incubation 50 μM for 1 h resulted morphological structural changes consistent apoptosis more than 60% present culture. significantly...
Abstract Parkinson’s disease (PD) is a progressive neurodegenerative with limited treatment options. Therefore, the identification of therapeutic targets urgently needed. Previous studies have shown that ligand activation sigma-1 chaperone (Sigma1R) promotes neuroprotection. The multitarget drug afobazole (5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole dihydrochloride) was to interact Sigma1Rs and prevent decreases in striatal dopamine 6-hydroxydopamine (6-OHDA)-induced parkinsonism...
A large amount of clinical and experimental data suggest the involvement neurotrophins, in particular brain-derived neurotrophic factor (BDNF), depression pathogenesis. However, therapeutic use BDNF is limited because its instability biological fluids, poor blood-brain barrier (BBB) permeability, presence side effects. low-molecular-weight mimetic GSB-106, which a substituted dimeric dipeptide bis(N-monosuccinyl-L-seryl-L-lysine)hexamethylenediamide, was designed synthesized based on fourth...