Background: Anxiety and mood disorders are the most abundant mental health problems
worldwide. The commonly used in clinical practice anxiolytics are focused on pharmacological
modulation of brain GABA receptor system activity. As a rule, their use presents a wide spectrum
of clinical issues such as dependence, memory impairment and etc. There is an increasing appreciation
of the role of neuropeptides and bioactive lipids in the pathophysiology of mood and anxiety
disorders as “mild” agents. Heptapeptide Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro) exhibits prolonged
anti-anxiety and nootropic effects.
Objective: In this issue, we tried to find the molecular mechanisms which may underlie Selank antianxiety
Methods: The main method we used was the radioligand – receptor method of analysis. We also
used HPLC (to obtain and ensure reagents and Selank purity) and the methods of brain cells plasmatic
membranes isolation and following detection of protein concentration in membrane samples.
Results: It was shown that Selank affect the [3H]GABA binding as a positive allosteric modulator.
The joint action of Selank and some of benzodiazepines also regulates activity of [3H]GABA binding
in specific manner, which is not cumulative and differs from either substance individually. Selank
is able to block the modulatory activity of Diazepam and Olanzapine, the location of their and
peptide binding sites apparently not the same, but potentially may partially overlaps.
Conclusion: Thus, we hypothesized and showed that one of Selank anti-anxiety molecular mechanisms
can be associated with subtype selective concentration - dependent allosteric modulation of