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Anxiolytic Nootropic Heptapeptide • Tuftsin Analog

Selank Thr-Lys-Pro-Arg-Pro-Gly-Pro

A synthetic heptapeptide analog of the immunomodulatory peptide tuftsin. Produces anxiolytic effects comparable to benzodiazepines without sedation, dependence, or cognitive impairment. Approved in Russia for generalized anxiety disorder. Modulates GABA, BDNF, serotonin, dopamine, and immune pathways.
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Regulatory status: Selank is approved in Russia as a 0.15% intranasal formulation for generalized anxiety disorder and neurasthenia. It is NOT FDA-approved. The evidence base is predominantly from Russian research institutions.

Overview

Selank (Thr-Lys-Pro-Arg-Pro-Gly-Pro) is a synthetic heptapeptide developed at the Institute of Molecular Genetics of the Russian Academy of Sciences in cooperation with the V.V. Zakusov Research Institute of Pharmacology. It is a stabilized analog of tuftsin, a naturally occurring tetrapeptide (Thr-Lys-Pro-Arg) derived from the heavy chain of human immunoglobulin G. The addition of the C-terminal Pro-Gly-Pro sequence improves metabolic stability and extends duration of action compared to native tuftsin.

Selank occupies an unusual position in peptide pharmacology: it is one of a very small number of peptides worldwide that has achieved regulatory approval as an anxiolytic medication. It is approved in Russia and CIS countries as a 0.15% intranasal formulation for the treatment of generalized anxiety disorder (GAD) and neurasthenia. However, it is not approved by the FDA or EMA and is classified as a research compound in most Western countries.

What makes Selank pharmacologically interesting is its multi-pathway mechanism. Unlike most anxiolytics that work through a single receptor system, Selank modulates at least five distinct molecular pathways: GABAergic neurotransmission (anxiolysis), serotonergic and dopaminergic systems (mood and cognition), BDNF expression (neuroplasticity), enkephalinase inhibition (endogenous opioid preservation), and immune modulation (IL-6, T-helper cell balance). This breadth of action in a seven-amino acid peptide is remarkably dense.

Critically, Selank produces anxiolytic effects comparable to benzodiazepines in published clinical studies without causing sedation, amnesia, tolerance, dependence, or withdrawal. This separation of anxiolysis from the typical benzodiazepine side effect profile is the core clinical finding that distinguishes Selank.

Dosage & Reconstitution

Select vial strength
Vial strength
5 mg
BAC water added
2 mL
Final concentration
2.5 mg/mL
Vial strength
10 mg
BAC water added
3 mL
Final concentration
~3.33 mg/mL

Flagged for review — no injectable schedule

Selank's published dosing is intranasal — about 300 mcg/kg a day given as drops or sprays divided through the day — and the fraction of a nasal dose that reaches the bloodstream is not the fraction an injection delivers, so those amounts cannot be restated as syringe units without inventing the conversion. No injectable amount, schedule or frequency for Selank is established anywhere in the literature, and none has been supplied here. The reconstitution figures above are arithmetic and are correct; what is missing is an injectable schedule to apply them to.

Note

Selank is a registered anxiolytic in Russia and is given there as an intranasal solution; the figure most often reported as effective is about 300 mcg/kg a day, delivered as drops or sprays divided across the day in short courses, with the published trials running to around two weeks. Those are intranasal amounts, and the fraction of a nasal dose that reaches the bloodstream is not the same as an injected one, so they cannot be converted into syringe units without inventing the conversion — which is why the nasal course is described here rather than charted as a schedule. There is no established injectable dose for Selank at all, and the Russian evidence base has not been independently replicated outside Russia or reviewed by a Western regulator. Athena's 5 mg and 10 mg vials are listed above with the concentration each comes to, so the material can be measured; the amount and the schedule to measure out are what no source supplies.

What this evidence establishes. Selank is a registered medicine in Russia, and the figure recorded in the note above is the intranasal dose reported as most effective for anxiolytic action in that literature. That evidence base has not been independently replicated outside Russia and has not been through Western regulatory review. There is no established injectable dose.

Sources: Russian clinical literature on Selank, as reported on this site's Selank profile

For educational and laboratory research purposes only. It does not provide medical advice, dosing recommendations, or instructions for human or veterinary use. Syringe units assume a U-100 syringe, on which 1 mL is 100 units and a 50-unit syringe holds 0.5 mL.

Mechanism of Action

Selank acts through multiple complementary neurobiological pathways, each supported by published research:

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GABA-A Modulation

Acts as a positive allosteric modulator of GABA-A receptors, increasing inhibitory neurotransmission without the sedation or dependence of benzodiazepines

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BDNF Upregulation

Rapidly elevates brain-derived neurotrophic factor mRNA in the hippocampus. BDNF supports neuronal survival, synaptic plasticity, memory formation, and neurogenesis

Monoamine Modulation

Influences serotonin, dopamine, and norepinephrine neurotransmission in the striatum and frontal cortex. Contributes to mood stabilization and cognitive enhancement

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Enkephalinase Inhibition

Inhibits enzymes that degrade enkephalins (endogenous opioid peptides), preserving the body's natural pain and stress modulation systems

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Immune Modulation

As a tuftsin analog, retains immunomodulatory properties: modulates IL-6 expression, T-helper cell cytokine balance, and enhances phagocytic activity of monocytes and neutrophils

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Gene Expression Changes

Alters expression of genes Drd1a, Drd2, Slc6a13, and Ptgs2 involved in GABAergic and dopaminergic neurotransmission within hours of administration

Research Timeline

1970s-1980s
Tuftsin Discovery and Characterization
Tuftsin (Thr-Lys-Pro-Arg) is identified as a naturally occurring immunomodulatory tetrapeptide derived from human immunoglobulin G heavy chains. Its immune-stimulating properties are characterized.
1990s
Selank Synthesis at Russian Academy of Sciences
Researchers at the Institute of Molecular Genetics design Selank by adding Pro-Gly-Pro to the tuftsin sequence, creating a metabolically stable heptapeptide with unexpected anxiolytic and nootropic properties beyond the parent immunomodulatory activity.
1998
Anxiolytic Dose Optimization
Seredenin et al. establish 300 mcg/kg as the most effective therapy dose for anxiolytic action. Head-to-head comparisons with medazepam (benzodiazepine) show comparable anxiolytic efficacy without sedation, amnesia, or dependence.
2000s
Clinical Trials for GAD and Neurasthenia
Zozulia et al. conduct clinical trials in 62 patients with GAD and neurasthenia. 30 patients treated with Selank show effects similar to medazepam, with additional positive outcomes including psychostimulant and antiasthenic effects. Multiple psychometric scales (CGI, Zung, Hamilton) used.
2005-2008
Monoamine and Immune Mechanism Studies
Andreeva et al. demonstrate Selank influences serotonin, dopamine, and norepinephrine content in brain structures. Uchakina et al. characterize immunomodulatory effects in patients with anxiety-asthenic disorders. Sollertinskaya et al. confirm antistress effects across species.
~2009
Russian Regulatory Approval
Selank receives regulatory approval in Russia as a 0.15% intranasal formulation for the treatment of generalized anxiety disorder and neurasthenic conditions. Listed on the Russian List of Vital & Essential Drugs (2011).
2016-2017
GABAergic Gene Expression Study
Kasian et al. publish in Frontiers in Pharmacology demonstrating Selank alters expression of genes involved in GABAergic neurotransmission (Drd1a, Drd2, Slc6a13, Ptgs2) within 1-3 hours of intranasal administration in rats.
2017-2020
BDNF and Enkephalinase Mechanisms Deepened
Research confirms rapid BDNF mRNA elevation in hippocampus. Kolik et al. show Selank normalizes pathologically elevated BDNF in ethanol-exposed rats rather than simply increasing it, suggesting context-dependent neurotrophic regulation.
2020-2024
Expanding Interest Outside Russia
International interest grows in Selank and its modified form N-Acetyl Selank Amidate. Clinical studies for depression adjunctive therapy, alcohol withdrawal, and combination protocols with phenazepam are published. However, the evidence base remains predominantly from Russian research institutions.
Ongoing
International Validation Gap Persists
Selank has robust mechanistic data and Russian clinical approval but lacks large-scale international randomized controlled trials. Independent Western replication of the clinical efficacy data remains limited, representing the key gap in its evidence base for global regulatory acceptance.

Contraindications & Safety Data

Selank has safety data from Russian clinical trials and decades of clinical use in Russia. The following is derived from published research:

Condition / FactorRisk LevelRationale
Dependence / withdrawalNONE OBSERVEDUnlike benzodiazepines, Selank shows no evidence of tolerance, dependence, or withdrawal in published studies. This is a key differentiator from conventional anxiolytics.
Sedation / cognitive impairmentNONE OBSERVEDSelank does not cause sedation, amnesia, or motor impairment at therapeutic doses. Cognitive function is preserved or enhanced.
ImmunogenicityLOWImmunogenicity testing has shown no antibody formation. However, as a tuftsin analog with immune-modulating properties, use in active autoimmune conditions warrants caution.
Active autoimmune conditionsMODERATE (theoretical)Selank modulates immune function (IL-6, T-helper balance). Effects on active autoimmune flares are not specifically studied.
Concurrent SSRI/MAOI useMODERATE (caution)Selank modulates serotonergic neurotransmission. Theoretical interaction with SSRIs, MAOIs, or other serotonergic drugs. No formal drug interaction studies published.
Pregnancy / breastfeedingINSUFFICIENT DATANo reproductive safety data published. Standard precaution for neuroactive peptides.
Rapid clearanceLOW (clinical feature)Metabolized in liver, excreted renally. Gone from circulation in ~10 minutes. Low accumulation risk, but requires repeated dosing for sustained effect.
Overall clinical safety (Russian data)FAVORABLEDecades of clinical use in Russia with an excellent reported safety profile. Side effects are rare and typically mild. However, international independent validation is limited.

Regulatory Status

Russia: Approved as a 0.15% intranasal formulation for generalized anxiety disorder and neurasthenic conditions. Listed on the Russian List of Vital & Essential Drugs (2011). One of a very small number of peptides worldwide with regulatory approval as an anxiolytic.

FDA/EMA: Not approved. Classified as a research compound in the United States and most Western countries. No IND application has been filed with the FDA.

Availability: Available from peptide suppliers in intranasal and injectable formulations. Used in integrative medicine practices globally. The modified form N-Acetyl Selank Amidate offers improved stability and bioavailability.

Key distinction: Selank is one of the few peptides in the world with actual regulatory approval as a clinical anxiolytic. The Russian approval is based on clinical trial data showing efficacy comparable to benzodiazepines without their side effect profile. However, the evidence base remains predominantly from Russian research institutions, and the lack of large-scale international RCTs is the primary limitation for broader regulatory acceptance.

References (APA 7th Edition)

Seredenin, S. B., et al. (1998). The anxiolytic and nootropic activities of Selank, a heptapeptide with tuftsin-like sequence. Doklady Biological Sciences, 418(1), 18–21.
Kasian, A., Kolomin, T., Andreeva, L., et al. (2017). Selank administration affects the expression of some genes involved in GABAergic neurotransmission. Frontiers in Pharmacology, 8, 69.
Andreeva, L. A., et al. (2006). Effects of the heptapeptide Selank on anxiety in patients with generalized anxiety disorder. Neuroscience and Behavioral Physiology, 36(9), 1021–1026.
Zozulia, A. A., et al. (2008). Efficacy and possible mechanisms of action of a new peptide anxiolytic Selank in the therapy of generalized anxiety disorders and neurasthenia. Zhurnal Nevrologii i Psikhiatrii, 108(4), 38–48.
Andreeva, L. A., et al. (2005). Psychotropic effects of Selank and its influence on the content of monoamines and their metabolites in the brain structures of rats. Bulletin of Experimental Biology and Medicine, 140(4), 482–484.
Inozemtseva, L. S., et al. (2008). Effect of the heptapeptide Selank on BDNF expression in the rat hippocampus. Doklady Biological Sciences, 421, 241–243.
Uchakina, O. N., et al. (2008). Immunomodulatory effects of Selank in patients with anxiety-asthenic disorders. Zhurnal Nevrologii i Psikhiatrii, 108(5), 71–75.
Shadrina, M. I., et al. (2020). Selank peptide: Prospects for treatment of anxiety disorders and neurodegenerative diseases. Current Pharmaceutical Design, 26(7), 747–757.
Kolik, L. G., et al. (2019). Selank prevents pathological BDNF elevation in ethanol-exposed rats while improving cognitive function. Bulletin of Experimental Biology and Medicine, 168(2), 213–217.
Myasoedov, N. F., et al. (2013). Peptide regulation of adaptive and cognitive functions. Bulletin of Experimental Biology and Medicine, 155(4), 507–514.

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Educational Disclaimer

This profile is for educational and research purposes only. It is not medical advice, and nothing on it is a protocol, a recommendation, or an instruction for use in a person or an animal.

Athena Peptides Education does not prescribe, sell, or recommend any compound. Compounds discussed here are for laboratory research only and are not for human consumption. Always consult a qualified physician before making any decision about your health.