Selank is a synthetic heptapeptide based on the natural immunomodulatory tetrapeptide tuftsin (a fragment of the IgG heavy chain), with a Pro-Gly-Pro C-terminal extension added for stability. Registered as a medical drug in Russia in 2009 (nasal drops, 0.15%), it is approved for generalised anxiety disorder and neurasthenia. Unlike classical anxiolytics, Selank produces anxiolytic effects without sedation or muscle relaxation.
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Join TelegramSelank's anxiolytic activity is mediated primarily through the GABAergic system. A PMC study (2016, PMC4757669) investigated Selank's effects on 84 genes involved in GABAergic neurotransmission in rat frontal cortex. Of 77 detectable genes, 45 showed expression changes 1 hour post-administration — 25 of which overlapped with direct GABA administration effects.
The strong positive correlation between Selank's and GABA's gene expression profiles suggests Selank allosterically modulates GABA-A receptor affinity for endogenous GABA, rather than acting as a direct agonist. This may account for the observed anxiolytic-profile differences from classical benzodiazepines noted in preclinical data.
Beyond GABAergic activity, Selank modulates cytokine expression and neuroimmune signalling, increasing expression of genes encoding immunoglobulins and chemokines. This neuroimmune dimension is studied in research examining immune-neurological signalling interactions in stress models.
Benzodiazepines act as direct GABA-A receptor positive allosteric modulators, producing potent anxiolysis alongside sedation, muscle relaxation, and dependency risk. Selank's proposed mechanism — allosterically increasing GABA-A receptor affinity for endogenous GABA — suggests a more nuanced, physiological modulation without full receptor occupancy.
This mechanistic distinction is consistent with Selank's clinical profile: anxiolytic and nootropic effects documented without sedation, cognitive impairment, or muscle relaxation in clinical studies — properties that distinguish it from the benzodiazepine class pharmacologically.
Selank was formally registered in Russia in 2009 following completion of preclinical and clinical trials, making it one of very few synthetic peptides to have passed full regulatory drug approval in any jurisdiction. Clinical applications include GAD and neurasthenia.
Studies in primates with neurosis demonstrated pronounced antidepressant and antistress effects, with abolition of aggression and fear reactions in previously neurotised animals. Adverse events documented in clinical trials were limited — the most notable was a transient blood glucose elevation in diabetics in approximately 7% of patients.