Selank
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Apenas para Uso em Pesquisa
Estes produtos sao destinados exclusivamente a pesquisa laboratorial e nao se destinam ao uso medico. Nao sao aprovados pela FDA para diagnosticar, tratar, curar ou prevenir qualquer doenca. Ao adquirir, voce certifica que os produtos serao utilizados exclusivamente para pesquisa e nao para consumo humano ou animal.
Resumo da Pesquisa
25 Citacoes PubMedVisao Geral Selank (TP-7) e um(a) sintetico(a) heptapeptide with a sequencia Thr-Lys-Pro-Arg-Pro-Gly-Pro (TKPRPGP). It foi desenvolvido(a) por the Institute of Molecular Genetics do(a) Russian Academy of Sciences in cooperation com o(a) V.V. Zakusov Research Institute of Pharmacology.[2] Selank is derivado(a) de tuftsin (Thr-Lys-Pro-Arg), a naturally occurring tetrapeptide que constitui a fragment do(a) heavy chain of human immunoglobulin G (IgG). The C-terminal Pro-Gly-Pro extension renders a molecula significantly mais resistant to peptidase hidrolise.[1] In experimental contexts, Selank exibe anxiolytic and nootropic effects comparable to classical benzodiazepines (como diazepam) but sem their characteristic negativo(a) observations — sedation, muscle relaxation, amnesia, dependence, or withdrawal syndrome.[5][6] Regulatory records no(a) Russian Federation cite Selank's registration for research related to generalized anxiety disorders and neurasthenia.[3] It is not registered pelo(a) U.S. FDA, que has raised immunogenicity concerns related to manipulacao.[4] A notavel pharmacokinetic feature is its exceptional intranasal biodisponibilidade of 92.8% — rare for a peptide...
Selank — Dados de Pesquisa em Resumo
| Propriedade | Valor |
|---|---|
| Citacoes PubMed Referenciadas | 25 |
| Pesquisadores Colaboradores | 3 |
| Condicoes de Armazenamento | Armazene o pó liofilizado a 4°C. |
| Padrao de Pureza | ≥99% (HPLC verified, 3rd-party COA) |
| Apenas para Uso em Pesquisa | Nao destinado ao consumo humano. Apenas para uso em pesquisa. |
Compare Selank com Outros Peptideos
Visao Geral
Visao Geral
Selank (TP-7) e um(a) sintetico(a) heptapeptide with a sequencia Thr-Lys-Pro-Arg-Pro-Gly-Pro (TKPRPGP). It foi desenvolvido(a) por the Institute of Molecular Genetics do(a) Russian Academy of Sciences in cooperation com o(a) V.V. Zakusov Research Institute of Pharmacology.[2]
Selank is derivado(a) de tuftsin (Thr-Lys-Pro-Arg), a naturally occurring tetrapeptide que constitui a fragment do(a) heavy chain of human immunoglobulin G (IgG). The C-terminal Pro-Gly-Pro extension renders a molecula significantly mais resistant to peptidase hidrolise.[1]
In experimental contexts, Selank exibe anxiolytic and nootropic effects comparable to classical benzodiazepines (como diazepam) but sem their characteristic negativo(a) observations — sedation, muscle relaxation, amnesia, dependence, or withdrawal syndrome.[5][6]
Regulatory records no(a) Russian Federation cite Selank's registration for research related to generalized anxiety disorders and neurasthenia.[3] It is not registered pelo(a) U.S. FDA, que has raised immunogenicity concerns related to manipulacao.[4] A notavel pharmacokinetic feature is its exceptional intranasal biodisponibilidade of 92.8% — rare for a peptide compound.[7]
Mecanismo de Acao
Mecanismo de Acao
Dual Mechanism: GABA-A Modulation + Enkephalinase Inhibition
Selank possesses um(a) unico(a) dual mecanismo de acao distinguishing it from classical anxiolytics:
1. GABA-A Receptor Positive Allosteric Modulation
Selank acts como um(a) positivo(a) allosteric modulator (PAM) do(a) GABA-A receptor. Its binding site is distinto(a) de the classical benzodiazepine site, though partial overlap may exist.[8] This modulacao aprimora the affinity of o receptor for GABA, increasing inhibitory neurotransmission sem producing sedation, amnesia, or muscle relaxation.[5]
Selank administration significantly alters mRNA levels of GABA receptor subunits — Gabrb3, Gabre (epsilon), and Gabrq (theta) — assim como the GABA transporter Slc6a13 (GAT-2) no(a) frontal cortex. Dramatically, Gabre and Gabrq diminuiu aproximadamente 20-fold at 1 hour, enquanto Hcrt (orexin/hypocretin) diminuiu 25-fold then surged 128-fold by 3 hours.[9] This orexin rebound is hypothesized to explana ausencia de sedation typical of benzodiazepines.
2. Enkephalinase Inhibition
Selank competitively inibe enzymes responsavel por the degradacao of enkephalins (endogenous opioid peptides), incluindo aminopeptidases, carboxypeptidase H, and angiotensin-converting enzyme (ACE). The inhibitory effect has an IC50 of aproximadamente 15–20 μM in human serum assays.[10] This extends the meia-vida of Leu-enkephalin, potentiating the body's natural stress-limiting and analgesic pathways.[11]
BDNF/TrkB Signaling
Selank rapidly elevates expression of Brain-Derived Neurotrophic Factor (BDNF) e seu(sua) receptor TrkB. An increase in Bdnf mRNA is observado(a) no(a) hippocampus as precoce as 90 minutes, with protein levels increasing by 24 hours.[12]
Monoamine Neurotransmitter Modulation
Selank induz region-specific changes in monoamine metabolismo:
- Serotonin: Increased 5-HIAA (metabolite) in hypothalamus and brainstem within 30 minutes to 2 hours[13]
- Norepinephrine: Increased no(a) hypothalamus[13]
- Dopamine: Strain-dependent — diminuiu metabolites in high-anxiety (BALB/c) mice, aumentou in low-anxiety (C57BL/6) mice[13]
Immunomodulacao
Selank modula IL-6 expression, normalizes the Th1/Th2 cytokine balance, and induz interferon-alpha (IFN-α) secretion.[14]
Receptor Selectivity
Importante, radioreceptor assays show que Selank does not directly displace ligands from benzodiazepine, dopamine (D2), serotonin (5-HT2), or opioid (μ, δ) receptors. Its effects on these systems are downstream or allosteric.[8] No entanto, the opioid antagonist naloxone bloqueia Selank's anxiolytic effects, confirming the enkephalin system's involvement.[15]
Aplicacoes de Pesquisa
Aplicacoes de Pesquisa
In laboratory research, Selank is investigated in multiplos(as) experimental paradigms:
- Anxiety and Generalized Anxiety Models — Registered no(a) Russian Federation for research related to generalized anxiety disorders and neurasthenia. Experimental readouts demonstrate anxiolytic effects comparable to benzodiazepines sem sedation, dependence, or withdrawal.[5][6]
- Cognitive Enhancement / Nootropic Paradigms — Studied for effects on memory consolidation and learning. A single injection aumentou memory trace stability for up to 30 days via serotonin metabolismo ativacao.[13]
- Alcohol Withdrawal Models — Eliminated withdrawal-induziu anxiety (EPM open arm time p<0.01), preveniu mechanical allodynia, and regulou BDNF content in hippocampus and prefrontal cortex.[16]
- Opioid Withdrawal Models — Reduced mean morphine withdrawal index by 39.6%, significantly attenuating convulsive reactions, ptosis, and posture disorders (p<0.0001). Increased tactile sensitivity threshold 9-fold.[17]
- Immunomodulacao and Antiviral Activity — Demonstrated antiviral effects against Influenza A (H3N2) ambos(as) in vivo e em vitro. Induced IFN-α secretion and normalized Th1/Th2 cytokine balance.[14]
- Gene Expression Modulation — Administration altered expression of 45 genes at 1 hour in frontal cortex, incluindo GABAergic receptor subunits and orexin/hypocretin (128-fold rebound at 3 hours).[9]
- Gastric Protection Models — Exhibited protective effects against stress- and ethanol-induziu gastric da mucosa injury, increasing da mucosa resistance to ulcerogenic factors.[2]
- Gut Microbiota and Stress — Prevented stress-induziu diminui in obligate microflora, reduziu corticosterone levels, and atenuou colon wall pathomorphological changes.[18]
Caracteristicas Bioquimicas
| Propriedade | Valor |
|---|---|
| Molecular Formula | C₃₃H₅₇N₁₁O₉ |
| Molecular Weight | 751.887 Da |
| CAS Number | 129954-34-3 |
| Sequence (3-Letter) | Thr-Lys-Pro-Arg-Pro-Gly-Pro |
| Sequence (1-Letter) | TKPRPGP |
| Amino Acids | 7 (heptapeptide) |
| Parent Molecule | Tuftsin (IgG fragment) + Pro-Gly-Pro stabilizer |
| Structural Type | Linear heptapeptide |
| Intranasal Bioavailability | 92.8% |
| Plasma Half-Life | ~2 minutes (effects persist 20-24 hours) |
Identificadores
| PubChem CID | |
|---|---|
| InChI Key | |
| Canonical SMILES | |
| IUPAC Name |
Resumo da Pesquisa Pre-clinica
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.
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Autores e Atribuicao
✍️ Autor do Artigo
Dr. Nikolay F. Myasoedov
Nikolay F. Myasoedov is affiliated com o(a) Institute of Molecular Genetics, Russian Academy of Sciences, e o(a) Department of Chemistry of Physiologically Active Compounds. He headed the research team que developed Selank (and the related compound Semax) as synthetic peptides based on natural regulatory peptides. His work covers enkephalinase inibicao, GABAergic mechanisms, expressao genica effects, e o(a) pharmacokinetics of proline-containing peptides. Nikolay F. Myasoedov é referenciado(a) como um(a) dos(as) principais cientistas envolvidos(as) na pesquisa e desenvolvimento de Selank. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →🎓 Autor de Revista Cientifica
Dr. Larisa G. Kolik
Larisa G. Kolik is a researcher no(a) V.V. Zakusov Research Institute of Pharmacology, Russian Academy of Medical Sciences. Her research focuses no(a) behavioral pharmacology of Selank, specifically regarding its efficacy in addiction models. She has extensively studied Selank's ability para atenuar withdrawal symptoms associado(a) com alcohol and morphine, e seu(sua) potential para proteger against memory impairment induzido(a) por cronico(a) alcohol exposure through BDNF regulacao. Larisa G. Kolik é referenciado(a) como um(a) dos(as) principais cientistas envolvidos(as) na pesquisa e desenvolvimento de Selank. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →Dr. Larisa G. Kolik is being referenced as one of the leading scientists involved in the research and development of Selank. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
🔬 Pesquisador Colaborador
Dr. Timur A. Kolomin
Timur A. Kolomin is affiliated com o(a) Department of Molecular Basis of Human Genetics no(a) Institute of Molecular Genetics, Russian Academy of Sciences. He specializes no(a) genomic effects of Selank, utilizing microarray technology to analyze how Selank administration affects transcriptome profiles no(a) hippocampus and spleen. He has identificado(a) specific genes envolveu in GABAergic neurotransmission, inflamacao, and ion homeostasis que are modulado(a) por Selank. Timur A. Kolomin é referenciado(a) como um(a) dos(as) principais cientistas envolvidos(as) na pesquisa e desenvolvimento de Selank. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →Dr. Timur A. Kolomin is being referenced as one of the leading scientists involved in the research and development of Selank. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
Citacoes Referenciadas
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.
DOIVyunova 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.
PubMedMedvedev 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.
PubMedU.S. Food and Drug Administration. Substancia Farmaceutica a Granels Used in Compounding Under Section 503B. FDA Compounding Database. 2023.
FDA.govZozulya 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.
PubMedKozlovskii 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.
PubMedKolomin 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.
DOIV'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.
DOIVolkova 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.
PubMedKost 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.
DOIZozulya 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.
PubMedInozemtseva 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.
PubMedNarkevich 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.
PubMedUchakina 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.
PubMedKozlovskii 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.
PubMedKolik 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.
PubMedKonstantinopolsky 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.
PubMedMukhina AY, et al. Effects of Selank on intestinal microbiota and stress-induziu changes. Russian Journal of Physiology. 2019/2020.
PubMedKasian 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.
PubMedKolik 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.
PubMedMedvedev 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.
PubMedSemenova 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.
PubMedFilatova 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.
PubMedKolomin 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.
PubMedAndreeva LA, Nagaev IY, Mezentseva MV, et al. Antiviral properties of structural fragments of o peptideo Selank. Doklady Biological Sciences. 2010;431:79–82.
PubMedAviso de Uso em Pesquisa
Apenas para Uso em Pesquisa (RUO). Nao destinado ao consumo humano, uso clinico, ou como medicamento, alimento, cosmetico ou dispositivo medico. Este produto nao foi avaliado pelo FDA e e fornecido exclusivamente para pesquisa laboratorial in vitro por profissionais qualificados.
Certificado de Analise
Each lot is independently tested by accredited third-party laboratories (ISO 17025) at 99%+ purity.
Ultimo Relatorio de Laboratorio
Armazenamento e Manuseio
Resumo
Armazene o pó liofilizado a 4°C. Solução reconstituída: 2-8°C, estável ~1 mês. Evite agitação.
Condições Recomendadas de Armazenamento Laboratorial
Liofilizado Powder: Store at 4°C (39°F) protegeu from light and moisture. Stable por períodos prolongados under these conditions.
Reconstituted Solution: Após reconstituição with agua bacteriostatica, refrigerate at 2–8°C. Stable for aproximadamente 1 month. Não congele.
Handling: Avoid vigorous shaking or agitation during reconstitution — direto(a) solvent gently down the side do(a) vial para prevenir peptide degradacao.
“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.”
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