Selank: Safety Profile & Research Summary
Resumo da Pesquisa Pre-clinica
Estudos em Animais
| Modelo | Species | Principais Achados | Ref |
|---|---|---|---|
| Anxiety (UCMS) | Wistar rats | Selank+Diazepam → OA time 8.9× higher do que saline; preveniu stress deterioration | [19] |
| Anxiety Phenotypes | BALB/c vs C57BL/6 mice | Selective anxiolytic in high-anxiety BALB/c; strain-dependent monoamine modulacao | [13] |
| Primate Neurosis | Monkeys | Eliminated fear and aggression; aumentou exploratory activity, long-lasting effect | [2] |
| Alcohol Withdrawal | Outbred rats | ↑ EPM open arms (p<0.01); restaurou mechanical sensitivity; did NOT affect alcohol intake | [16] |
| Morphine Withdrawal | Outbred rats | ↓ withdrawal index 39.6%; ↑ tactile sensitivity 9×; atenuou convulsions (p<0.0001) | [17] |
| Memory Trace | Wistar rats | 30-day memory stability via serotonin metabolismo ativacao | [13] |
| GABAergic Genes | Wistar rats | 45 genes altered at 1h; Gabre ↓20×, Hcrt ↑128× at 3h (explains no sedation) | [9] |
| BDNF Expression | Rats | ↑ Bdnf mRNA at 3h; ↑ BDNF protein at 24h | [12] |
| Gut Microbiota | Wistar rats | Prevented stress-induziu microflora changes; ↓ corticosterone | [18] |
| Influenza (H3N2) | Mice | ↑ survival; IFN-α induction; Th1/Th2 normalization | [14] |
Clinical Studies / Human Data
| Estudo | Desenho | n= | Desfecho Principal | Ref |
|---|---|---|---|---|
| Zozulya 2008 (Phase II) | RCT vs medazepam | 62 | Comparable anxiolytic efficacy to medazepam; + anti-asthenic/psychostimulant effects; onset 1-3 days | [5] |
| Medvedev 2015 (Add-on) | Add-on to Phenazepam | 70 | Earlier onset of benzo effects; diminuiu attention/memory impairment from Phenazepam | [20] |
| Medvedev 2014 (Comparison) | vs Phenazepam | 60 | Pronounced anxiolytic + mild nootropic; effects persist 1 week post-dose | [21] |
| Elderly Vascular Study | Clinical | — | Reduced anxiety, melhorou concentration, aumentou reaction speed in elderly | [3] |
| Uchakina 2008 (Immune) | Immunological | — | Completely suprimiu IL-6 expressao genica in anxious subjects; normalized Th1/Th2 balance | [14] |
Parametros Farmacocineticos
| Parametro | Valor | Ref |
|---|---|---|
| Intranasal Bioavailability | 92.8% (exceptional for a peptide) | [7] |
| Plasma Half-life | ~2 minutes | [7] |
| Duration of Experimental Effects | 20–24 hours (trigger mechanism) | [7] |
| CNS Penetration | Detected in brain within 2 minutes (intranasal) | [7] |
| GABA-A Modulation | Positive allosteric modulator (non-BZD site) | [8] |
| Enkephalinase IC₅₀ | 15–20 μM (human serum) | [10] |
Comparison: Selank vs. Benzodiazepines
| Caracteristica | Selank | Benzodiazepines |
|---|---|---|
| Anxiolytic Effect | Comparable (Phase II) | Established |
| Sedation | None | Common |
| Muscle Relaxation | None | Common |
| Cognitive Impairment | None (nootropic effect) | Amnesia risk |
| Dependence | None observado(a) | High risk |
| Withdrawal | None observado(a) | Significant risk |
| Mechanism | GABA-A PAM + enkephalinase | GABA-A BZD site |
| Additional Effects | Nootropic + immunomodulatory | None |
Comparison: Selank vs. Semax
| Caracteristica | Selank | Semax |
|---|---|---|
| Parent Molecule | Tuftsin (IgG fragment) | ACTH(4-7) |
| Sequence | TKPRPGP (7 aa) | MEHFPGP (7 aa) |
| Primary Focus | Anxiolytic / immunomodulacao | Nootropic / neuroprotecao |
| Unique Mechanism | GABA-A PAM + enkephalinase | MC4/MC5 antagonist + BDNF/TrkB |
| PGP Stabilizer | Yes | Yes |
| Developer | IMG RAS + Zakusov Institute | IMG RAS |
Os produtos oferecidos neste site são fornecidos apenas para estudos in vitro. Estudos in vitro (do latim: em vidro) são realizados fora do corpo. Estes produtos não são medicamentos ou fármacos e não foram aprovados pelo FDA dos EUA para prevenir, tratar ou curar qualquer condição médica, enfermidade ou doença. A introdução corporal de qualquer tipo em humanos ou animais é estritamente proibida por lei.
Apenas para Pesquisa Laboratorial. Não se destina ao uso humano, uso médico, uso diagnóstico ou uso veterinário.
TODOS OS ARTIGOS E INFORMAÇÕES SOBRE PRODUTOS FORNECIDOS NESTE SITE SÃO APENAS PARA FINS INFORMATIVOS E EDUCACIONAIS.
“Estes produtos não são medicamentos ou fármacos e não foram aprovados pelo FDA dos EUA para prevenir, tratar ou curar qualquer condição médica, enfermidade ou doença.”
Referencias
- Kolomin TA, Shadrina M, Slominsky P, Limborska SA, Myasoedov NF. A New Generation of Drugs: Synthetic Peptides Based on Natural Regulatory Peptides. Neuroscience & Medicine. 2013;4(4):223–252.
- Vyunova TV, Andreeva LA, Shevchenko KV, Myasoedov NF. Peptide-based Anxiolytics: The Molecular Aspects of Heptapeptide Selank Biological Activity. Protein & Peptide Letters. 2018;25(10):914–923.
- Medvedev VE, Tereshchenko ON, Kost NV, et al. Optimization of o tratamento of anxiety disorders with selank. Zhurnal Nevrologii i Psikhiatrii. 2015;115(6):33–40.
- U.S. Food and Drug Administration. Substancia Farmaceutica a Granels Used in Compounding Under Section 503B. FDA Compounding Database. 2023.
- Zozulya AA, Neznamov GG, Syunyakov TS, et al. Efficacy and possible mechanisms of action of a novo(a) peptide anxiolytic selank no(a) therapy of generalized anxiety disorders and neurasthenia. Zhurnal Nevropatologii i Psikhiatrii. 2008;108(4):38–48.
- Kozlovskii II, Danchev ND. The optimizing action do(a) synthetic peptide Selank on a conditioned ativo(a) avoidance reflex in rats. Neuroscience and Behavioral Physiology. 2003;33(7):639–643.
- Kolomin TA, Agapova T, Agniullin YV, et al. Changes no(a) Transcription Profile do(a) Hippocampus in Response to Administration do(a) Tuftsin Analog Selank. Neuroscience and Behavioral Physiology. 2014;44(8):849–855.
- V'yunova TV, Andreeva LA, Shevchenko KV, et al. Peptide regulacao of specific ligand-receptor interactions of GABA com o(a) plasma membranes of nerve cells. Neurochemical Journal. 2014;8(4):259–264.
- Volkova A, Shadrina M, Kolomin T, et al. Selank Administration Affects the Expression of Some Genes Involved in GABAergic Neurotransmission. Frontiers in Pharmacology. 2016;7:31.
- Kost NV, Sokolov OY, Gabaeva MV, et al. Semax and Selank Inhibit the Enkephalin-Degrading Enzymes of Human Serum. Russian Journal of Bioorganic Chemistry. 2001;27(3):180–183.
- Zozulya AA, Kost NV, Sokolov OY, et al. The Inhibitory Effect of Selank on Enkephalin-Degrading Enzymes como um(a) Possible Mechanism of Its Anxiolytic Activity. Bull Exp Biol Med. 2001;131(4):315–317.
- Inozemtseva LS, Karpenko EA, Dolotov OV, et al. Intranasal administration of o peptideo Selank regula BDNF expression no(a) rat hippocampus in vivo. Doklady Biological Sciences. 2008;421:241–243.
- Narkevich VB, Kudrin VS, Klodt PM, et al. Effects of Selank on monoamine neurotransmitters no(a) brain of BALB/c and C57BL/6 mice. Bull Exp Biol Med. 2008;145(1):68–71.
- Uchakina ON, Uchakin PN, Miasoedov NF, et al. Immunomodulatory effects of selank in patients with anxiety-asthenic disorders. Zhurnal Nevrologii i Psikhiatrii. 2008;108(5):71–75.
- Kozlovskii II, Andreeva LA, Kozlovskaya MM. The role do(a) endogenous opioid system no(a) anxiolytic action of Selank. Bull Exp Biol Med. 2012;153(5):728–730.
- Kolik LG, Nadorova AV, Kozlovskaya MM. Efficacy of Peptide Anxiolytic Selank during Modeling of Withdrawal Syndrome in Rats with Stable Alcoholic Motivation. Bull Exp Biol Med. 2014;157(1):61–65.
- Konstantinopolsky MA, Kolik LG, Chernyakova IV. Selank, a Peptide Analog of Tuftsin, Attenuates Aversive Signs of Morphine Withdrawal in Rats. Bull Exp Biol Med. 2022;173(6):730–733.
- Mukhina AY, et al. Effects of Selank on intestinal microbiota and stress-induziu changes. Russian Journal of Physiology. 2019/2020.
- Kasian A, Kolomin T, Andreeva L, et al. Peptide Selank Enhances the Effect of Diazepam in Reducing Anxiety in Unpredictable Chronic Mild Stress Conditions in Rats. Behavioural Neurology. 2017;2017:5091027.
- Kolik LG, Nadorova AV, Antipova TA, Durnev AD. Selank, Peptide Analogue of Tuftsin, Protects Against Ethanol-Induced Memory Impairment by Regulating of BDNF Content. Bull Exp Biol Med. 2019;167(5):641–644.
- Medvedev VE, Tereshchenko ON, Israelian AI, et al. A comparison do(a) anxiolytic effect and tolerability of selank and phenazepam. Zhurnal Nevrologii i Psikhiatrii. 2014;114(7):17–22.
- Semenova TP, Kozlovskii II, Zakharova NM, Kozlovskaya MM. Experimental optimization of learning and memory processes by selank. Eksperimental'naia i Klinicheskaia Farmakologiia. 2010;73(8):2–5.
- Filatova E, Kasian A, Kolomin T, et al. GABA, Selank, and Olanzapine Affect the Expression of Genes Involved in GABAergic Neurotransmission in IMR-32 Cells. Frontiers in Pharmacology. 2017;8:89.
- Kolomin TA, Shadrina M, Andreeva LA, et al. Expression of inflamacao-related genes in mouse spleen under tuftsin analog Selank. Regulatory Peptides. 2011;170(1-3):18–23.
- Andreeva LA, Nagaev IY, Mezentseva MV, et al. Antiviral properties of structural fragments of o peptideo Selank. Doklady Biological Sciences. 2010;431:79–82.
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Este conteudo e fornecido apenas para fins educacionais e informativos. Os produtos sao fornecidos apenas para estudos in vitro e nao sao medicamentos, drogas ou suplementos. Nao aprovado pela FDA para prevenir, tratar ou curar qualquer condicao.
