The inhibitory effect of Selank on enkephalin-degrading enzymes as a possible mechanism of its anxiolytic activity.
Zozulya. A A AA; Kost. N V NV; Yu Sokolov. O O; Gabaeva. M V MV; Grivennikov. I A IA; Andreeva. L N LN; Zolotarev. Y A YA; Ivanov. S V SV; Andryushchenko. A V AV; Myasoedov. N F NF; Smulevich. A B AB
Key Findings
- Generalized anxiety patients have faster enkephalin breakdown and lower natural enzyme inhibitors.
- Selank doseâdependently inhibits plasma enkephalinâdegrading enzymes (IC50 â15âŻÂ”M).
- Selank is more potent than traditional peptidase inhibitors like bacitracin and puromycin.
Practical Outcomes
- Selank may be a promising supplement for managing anxiety by preserving enkephalins, offering a potentially safer alternative to classic anxiolytics. Biohackers could consider it for experimental use, but should await clearer dosing guidelines and safety data before routine adoption.
Summary
Selank is a small peptide that can calm anxiety by stopping the breakdown of natural brain chemicals called enkephalins. In people with generalized anxiety, enkephalins break down faster, but Selank blocks the enzymes that do this, and it does so more effectively than some other enzyme blockers. This suggests Selank could be a useful, lowâsideâeffect option for anxiety, though exact dosing for everyday use isnât defined yet.
Abstract
Examination of patients with various forms of anxiety and phobic disorders (according to DSM-4 criteria) demonstrated a considerable shortening of enkephalin half-life and reduced total enkephalinase activity in the blood during generalized anxiety, but not during panic disorders and agoraphobia. This was probably related to low blood concentration of endogenous inhibitors of enkephalin-degrading enzymes in patients with generalized anxiety disorders. Heptapeptide Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro), which attenuates behavioral anxiety reactions and does not cause side effects typical of most anxiolytics, dose-dependently inhibited enzymatic hydrolysis of plasma enkephalin (IC50 15 microM). Selank was more potent than peptidase inhibitors bacitracin and puromycin in inhibiting enkephalinases. These results suggest that high efficiency of Selank in the therapy of anxiety and phobic disorders, including generalized anxiety, is due to its ability to inhibit enkephalin hydrolysis.
Study Information
pubmed
2001
10.1023/a:1017979514274