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Referências encontradas : 4733 [refinar]
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[PMID]:29274489
[Au] Autor:Salikov RF; Trainov KP; Belousova IK; Belyy AY; Fatkullina US; Mulyukova RV; Zainullina LF; Vakhitova YV; Tomilov YV
[Ad] Endereço:N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky Prospect, 119991 Moscow, Russian Federation.
[Ti] Título:Branching tryptamines as a tool to tune their antiproliferative activity.
[So] Source:Eur J Med Chem;144:211-217, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The influence of a series of tryptamine derivatives on the viability of normal (HEK293) and tumor (HepG2, Jurkat and SH-SY5Y) cells has been evaluated. All tryptamines tested were three different substitution types: C- and N-branching, and indole benzylation. All the derivations enhance the activity of compounds separately, although the effects of different substitutions were not additive. Thus, combinations of C- and N-branchings as well as C-branching and indole benzylation gave little or no increase in activity.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Proliferação Celular/efeitos dos fármacos
Triptaminas/química
Triptaminas/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Células HEK293
Seres Humanos
Indóis/química
Indóis/farmacologia
Neoplasias/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Indoles); 0 (Tryptamines)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171224
[St] Status:MEDLINE


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[PMID]:28466676
[Au] Autor:Backlund PS; Urbanski HF; Doll MA; Hein DW; Bozinoski M; Mason CE; Coon SL; Klein DC
[Ad] Endereço:Biomedical Mass Spectrometry Facility, Intramural Research Program.
[Ti] Título:Daily Rhythm in Plasma N-acetyltryptamine.
[So] Source:J Biol Rhythms;32(3):195-211, 2017 Jun.
[Is] ISSN:1552-4531
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Normal physiology undergoes 24-h changes in function that include daily rhythms in circulating hormones, most notably melatonin and cortical steroids. This study focused on N-acetyltryptamine, a little-studied melatonin receptor mixed agonist-antagonist and the likely evolutionary precursor of melatonin. The central issue addressed was whether N-acetyltryptamine is physiologically present in the circulation. N-acetyltryptamine was detected by LC-MS/MS in daytime plasma of 3 different mammals in subnanomolar levels (mean ± SEM: rat, 0.29 ± 0.05 nM, n = 5; rhesus macaque, 0.54 ± 0.24 nM, n = 4; human, 0.03 ± 0.01 nM, n = 32). Analysis of 24-h blood collections from rhesus macaques revealed a nocturnal increase in plasma N-acetyltryptamine (p < 0.001), which varied from 2- to 15-fold over daytime levels among the 4 animals studied. Related RNA sequencing studies indicated that the transcript encoding the tryptamine acetylating enzyme arylalkylamine N-acetyltransferase (AANAT) is expressed at similar levels in the rhesus pineal gland and retina, thereby indicating that either tissue could contribute to circulating N-acetyltryptamine. The evidence that N-acetyltryptamine is a physiological component of mammalian blood and exhibits a daily rhythm, together with known effects as a melatonin receptor mixed agonist-antagonist, shifts the status of N-acetyltryptamine from pharmacological tool to candidate for a physiological role. This provides a new opportunity to extend our understanding of 24-h biology.
[Mh] Termos MeSH primário: Ritmo Circadiano
Fotoperíodo
Triptaminas/sangue
[Mh] Termos MeSH secundário: Animais
Arilalquilamina N-Acetiltransferase/genética
Perfilação da Expressão Gênica
Seres Humanos
Macaca mulatta
Masculino
Melatonina/metabolismo
Glândula Pineal/enzimologia
Ratos
Retina/enzimologia
Espectrometria de Massas em Tandem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Tryptamines); 1016-47-3 (N-acetyltryptamine); EC 2.3.1.87 (Arylalkylamine N-Acetyltransferase); JL5DK93RCL (Melatonin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE
[do] DOI:10.1177/0748730417700458


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[PMID]:27773294
[Au] Autor:Maktedar SS; Mehetre SS; Avashthi G; Singh M
[Ad] Endereço:School of Chemical Sciences, Central University of Gujarat, Gandhinagar 382030, India. Electronic address: shrikantmaktedar@gmail.com.
[Ti] Título:In situ sonochemical reduction and direct functionalization of graphene oxide: A robust approach with thermal and biomedical applications.
[So] Source:Ultrason Sonochem;34:67-77, 2017 01.
[Is] ISSN:1873-2828
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The rapid, robust, scalable and non-hazardous sonochemical approach for in situ reduction and direct functionalization of graphene oxide has been developed for non-toxic biomedical applications. The graphene oxide (GrO) was directly functionalized with tryptamine (TA) without using any hazardous acylating and coupling reagents. The reaction was completed within 20min. An impact of ultrasound was inferred for a direct functionalization with other conventional methods. The evolved electronic states were confirmed with near edge X-ray absorption fine structure (NEXAFS). The direct covalent functionalization and formation of f-(TA) GrO was proven with FTIR, C solid state NMR, XPS, XRD, Raman' HRTEM, AFM and TGA. The total percentage weight loss in TGA confirms an enhanced thermal stability of f-(TA) GrO. The f-(TA) GrO was further explored for an investigation of in vitro antimicrobial activity to ensure the health and environmental safety. An outstanding antibacterial activity of f-(TA) GrO was found against gram positive Staphylococcus aureus at MIC 128mgmL . It confirms a suitability of f-(TA) GrO for thermally stable antibacterial coating. The f-(TA) GrO showed 39.14-48.9% antioxidant activities, evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical assay. The inherent cytotoxicity of f-(TA) GrO was evaluated with SRB assay to living cells, MCF-7 and Vero. The estimated cell viabilities were >80% upon addition of f-(TA) GrO over a wide concentration range of 10-80µgmL . The high cytocompatibility of f-(TA) GrO confirms the low toxicity and an excellent biocompatibility. The morphological effect on Vero cell line, evidently confirmed the biocompatibility of f-(TA) GrO. Therefore, f-(TA) GrO was emerged as an advanced functional biomaterial for thermal and biomedical applications.
[Mh] Termos MeSH primário: Grafite/química
Grafite/farmacologia
Óxidos/química
Temperatura Ambiente
Ondas Ultrassônicas
[Mh] Termos MeSH secundário: Animais
Antibacterianos/química
Antibacterianos/farmacologia
Antibacterianos/toxicidade
Cercopithecus aethiops
Depuradores de Radicais Livres/química
Depuradores de Radicais Livres/farmacologia
Depuradores de Radicais Livres/toxicidade
Grafite/toxicidade
Seres Humanos
Células MCF-7
Teste de Materiais
Testes de Sensibilidade Microbiana
Staphylococcus aureus/efeitos dos fármacos
Triptaminas/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Free Radical Scavengers); 0 (Oxides); 0 (Tryptamines); 422ZU9N5TV (tryptamine); 7782-42-5 (Graphite)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180131
[Lr] Data última revisão:
180131
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE


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[PMID]:29226741
[Au] Autor:González-Hernández A; Marichal-Cancino BA; MaassenVanDenBrink A; Villalón CM
[Ad] Endereço:a Instituto de Neurobiología , Universidad Nacional Autónoma de México , Querétaro , México.
[Ti] Título:Side effects associated with current and prospective antimigraine pharmacotherapies.
[So] Source:Expert Opin Drug Metab Toxicol;14(1):25-41, 2018 Jan.
[Is] ISSN:1744-7607
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Migraine is a neurovascular disorder. Current acute specific antimigraine pharmacotherapies target trigeminovascular 5-HT , 5-HT and CGRP receptors but, unfortunately, they induce some cardiovascular and central side effects that lead to poor treatment adherence/compliance. Therefore, new antimigraine drugs are being explored. Areas covered: This review considers the adverse (or potential) side effects produced by current and prospective antimigraine drugs, including medication overuse headache (MOH) produced by ergots and triptans, the side effects observed in clinical trials for the new gepants and CGRP antibodies, and a section discussing the potential effects resulting from disruption of the cardiovascular CGRPergic neurotransmission. Expert opinion: The last decades have witnessed remarkable developments in antimigraine therapy, which includes acute (e.g. triptans) and prophylactic (e.g. ß-adrenoceptor blockers) antimigraine drugs. Indeed, the triptans represent a considerable advance, but their side effects (including nausea, dizziness and coronary vasoconstriction) preclude some patients from using triptans. This has led to the development of the ditans (5-HT receptor agonists), the gepants (CGRP receptor antagonists) and the monoclonal antibodies against CGRP or its receptor. The latter drugs represent a new hope in the antimigraine armamentarium, but as CGRP plays a role in cardiovascular homeostasis, the potential for adverse cardiovascular side effects remains latent.
[Mh] Termos MeSH primário: Desenho de Drogas
Transtornos de Enxaqueca/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Anticorpos Monoclonais/administração & dosagem
Anticorpos Monoclonais/efeitos adversos
Anticorpos Monoclonais/farmacologia
Transtornos da Cefaleia Secundários/etiologia
Seres Humanos
Transtornos de Enxaqueca/fisiopatologia
Receptores de Peptídeo Relacionado com o Gene de Calcitonina/antagonistas & inibidores
Receptores de Peptídeo Relacionado com o Gene de Calcitonina/metabolismo
Receptores de Serotonina/efeitos dos fármacos
Receptores de Serotonina/metabolismo
Agonistas de Receptores de Serotonina/administração & dosagem
Agonistas de Receptores de Serotonina/efeitos adversos
Agonistas de Receptores de Serotonina/farmacologia
Triptaminas/administração & dosagem
Triptaminas/efeitos adversos
Triptaminas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Antibodies, Monoclonal); 0 (Receptors, Calcitonin Gene-Related Peptide); 0 (Receptors, Serotonin); 0 (Serotonin Receptor Agonists); 0 (Tryptamines); 0 (serotonin 1F receptor)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE
[do] DOI:10.1080/17425255.2018.1416097


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[PMID]:29174963
[Au] Autor:Hoffmann J; May A
[Ad] Endereço:Department of Systems Neuroscience, University Medical Center Hamburg-Eppendorf, Hamburg, Germany.
[Ti] Título:Diagnosis, pathophysiology, and management of cluster headache.
[So] Source:Lancet Neurol;17(1):75-83, 2018 Jan.
[Is] ISSN:1474-4465
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Cluster headache is a trigeminal autonomic cephalalgia characterised by extremely painful, strictly unilateral, short-lasting headache attacks accompanied by ipsilateral autonomic symptoms or the sense of restlessness and agitation, or both. The severity of the disorder has major effects on the patient's quality of life and, in some cases, might lead to suicidal ideation. Cluster headache is now thought to involve a synchronised abnormal activity in the hypothalamus, the trigeminovascular system, and the autonomic nervous system. The hypothalamus appears to play a fundamental role in the generation of a permissive state that allows the initiation of an episode, whereas the attacks are likely to require the involvement of the peripheral nervous system. Triptans are the most effective drugs to treat an acute cluster headache attack. Monoclonal antibodies against calcitonin gene-related peptide, a crucial neurotransmitter of the trigeminal system, are under investigation for the preventive treatment of cluster headache. These studies will increase our understanding of the disorder and perhaps reveal other therapeutic targets.
[Mh] Termos MeSH primário: Anestésicos Locais/farmacologia
Cefaleia Histamínica/tratamento farmacológico
Cefaleia Histamínica/etiologia
Cefaleia Histamínica/fisiopatologia
Lidocaína/farmacologia
Oxigênio/farmacologia
Triptaminas/farmacologia
[Mh] Termos MeSH secundário: Anestésicos Locais/administração & dosagem
Cefaleia Histamínica/diagnóstico
Seres Humanos
Lidocaína/administração & dosagem
Oxigênio/administração & dosagem
Triptaminas/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Tryptamines); 98PI200987 (Lidocaine); S88TT14065 (Oxygen)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171227
[Lr] Data última revisão:
171227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE


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[PMID]:28459438
[Au] Autor:Li Y; Lucas-Osma AM; Black S; Bandet MV; Stephens MJ; Vavrek R; Sanelli L; Fenrich KK; Di Narzo AF; Dracheva S; Winship IR; Fouad K; Bennett DJ
[Ad] Endereço:Neuroscience and Mental Health Institute and Faculty of Rehabilitation Medicine, University of Alberta, Edmonton, Alberta, Canada.
[Ti] Título:Pericytes impair capillary blood flow and motor function after chronic spinal cord injury.
[So] Source:Nat Med;23(6):733-741, 2017 Jun.
[Is] ISSN:1546-170X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Blood vessels in the central nervous system (CNS) are controlled by neuronal activity. For example, widespread vessel constriction (vessel tone) is induced by brainstem neurons that release the monoamines serotonin and noradrenaline, and local vessel dilation is induced by glutamatergic neuron activity. Here we examined how vessel tone adapts to the loss of neuron-derived monoamines after spinal cord injury (SCI) in rats. We find that, months after the imposition of SCI, the spinal cord below the site of injury is in a chronic state of hypoxia owing to paradoxical excess activity of monoamine receptors (5-HT ) on pericytes, despite the absence of monoamines. This monoamine-receptor activity causes pericytes to locally constrict capillaries, which reduces blood flow to ischemic levels. Receptor activation in the absence of monoamines results from the production of trace amines (such as tryptamine) by pericytes that ectopically express the enzyme aromatic L-amino acid decarboxylase (AADC), which synthesizes trace amines directly from dietary amino acids (such as tryptophan). Inhibition of monoamine receptors or of AADC, or even an increase in inhaled oxygen, produces substantial relief from hypoxia and improves motoneuron and locomotor function after SCI.
[Mh] Termos MeSH primário: Monoaminas Biogênicas/metabolismo
Capilares/metabolismo
Hipóxia/metabolismo
Locomoção/fisiologia
Pericitos/metabolismo
Traumatismos da Medula Espinal/metabolismo
Vasoconstrição
[Mh] Termos MeSH secundário: Animais
Descarboxilases de Aminoácido-L-Aromático/metabolismo
Capilares/efeitos dos fármacos
Capilares/patologia
Capilares/fisiopatologia
Injeções Espinhais
Locomoção/efeitos dos fármacos
Microscopia Confocal
Microscopia de Interferência
Norepinefrina/metabolismo
Oxigênio/metabolismo
Oxigenoterapia
RNA Mensageiro/metabolismo
Ratos
Receptor 5-HT1B de Serotonina/metabolismo
Receptores Adrenérgicos alfa 2/metabolismo
Receptores 5-HT1 de Serotonina/metabolismo
Serotonina/metabolismo
Antagonistas do Receptor 5-HT1 de Serotonina/farmacologia
Traumatismos da Medula Espinal/patologia
Traumatismos da Medula Espinal/fisiopatologia
Transcriptoma
Triptaminas/metabolismo
Tiramina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biogenic Monoamines); 0 (RNA, Messenger); 0 (Receptor, Serotonin, 5-HT1B); 0 (Receptors, Adrenergic, alpha-2); 0 (Receptors, Serotonin, 5-HT1); 0 (Serotonin 5-HT1 Receptor Antagonists); 0 (Tryptamines); 333DO1RDJY (Serotonin); 422ZU9N5TV (tryptamine); EC 4.1.1.28 (Aromatic-L-Amino-Acid Decarboxylases); S88TT14065 (Oxygen); X4W3ENH1CV (Norepinephrine); X8ZC7V0OX3 (Tyramine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171206
[Lr] Data última revisão:
171206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE
[do] DOI:10.1038/nm.4331


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[PMID]:28749698
[Au] Autor:Raffaelli B; Israel H; Neeb L; Reuter U
[Ad] Endereço:a Department of Neurology , Charité Universitätsmedizin Berlin , Berlin , Germany.
[Ti] Título:The safety and efficacy of the 5-HT 1F receptor agonist lasmiditan in the acute treatment of migraine.
[So] Source:Expert Opin Pharmacother;18(13):1409-1415, 2017 Sep.
[Is] ISSN:1744-7666
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Migraine is among the most disabling disorders worldwide, with a significant therapeutic need. Triptans are drugs of choice in the acute attack treatment, but they are contraindicated in patients with vascular conditions due to their potential vasoconstrictive properties. Further limitations include side effects, inconsistency in therapeutic action and possible non-response. Lasmiditan, a highly selective 5-HT1F receptor agonist, is a novel acute anti-migraine substance devoid of vasoconstriction. Areas covered: This article reviews the clinical efficacy and safety of oral and intravenous lasmiditan as a possible acute migraine treatment. We analyze all currently available results in Phase I to III studies. Expert opinion: Lasmiditan is a promising acute migraine therapy, in particular for patients at cardiovascular risk. Phase II and the first Phase III clinical trials show a significant better headache response in comparison to placebo. The efficacy of lasmiditan proves that vasoconstriction is not essential for acute migraine therapy and thereby points, in addition to a well-established trigeminal contribution, to central neuronal mechanisms in migraine pathophysiology. Lasmiditan penetrates the blood-brain barrier and CNS associated adverse events are common, but mostly in mild to moderate severity. The results of long-term Phase III studies will determine if these adverse events represent a limitation in clinical practice.
[Mh] Termos MeSH primário: Benzamidas/uso terapêutico
Transtornos de Enxaqueca/tratamento farmacológico
Piperidinas/uso terapêutico
Piridinas/uso terapêutico
Receptores de Serotonina/metabolismo
Agonistas de Receptores de Serotonina/uso terapêutico
[Mh] Termos MeSH secundário: Benzamidas/administração & dosagem
Benzamidas/efeitos adversos
Doenças Cardiovasculares/induzido quimicamente
Ensaios Clínicos Fase III como Assunto
Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/etiologia
Seres Humanos
Piperidinas/administração & dosagem
Piperidinas/efeitos adversos
Piridinas/administração & dosagem
Piridinas/efeitos adversos
Fatores de Risco
Agonistas de Receptores de Serotonina/administração & dosagem
Agonistas de Receptores de Serotonina/efeitos adversos
Resultado do Tratamento
Triptaminas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (2,4,6-trifluoro-N-(6-((1-methylpiperidin-4-yl)carbonyl)pyridin-2yl)benzamide); 0 (Benzamides); 0 (Piperidines); 0 (Pyridines); 0 (Receptors, Serotonin); 0 (Serotonin Receptor Agonists); 0 (Tryptamines); 0 (serotonin 1F receptor)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171204
[Lr] Data última revisão:
171204
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE
[do] DOI:10.1080/14656566.2017.1361406


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[PMID]:28806604
[Au] Autor:Berger A; Tanuhadi E; Brecker L; Schinnerl J; Valant-Vetschera K
[Ad] Endereço:Chemodiversity Research Group, Department of Botany and Biodiversity Research, University of Vienna, Rennweg 14, A-1030, Vienna, Austria. Electronic address: andi.berger@univie.ac.at.
[Ti] Título:Chemodiversity of tryptamine-derived alkaloids in six Costa Rican Palicourea species (Rubiaceae-Palicoureeae).
[So] Source:Phytochemistry;143:124-131, 2017 Nov.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We report 14 harmala and tryptamine-iridoid alkaloids with various tri-, tetra- and pentacyclic cores from leaves and stem bark of six species of the large and complex neotropical genus Palicourea. Among them is the previously undescribed compound deoxostrictosamide which is related to strictosamide, a key intermediate in camptothecin biosynthesis. In addition, we describe the occurrence of 1,2,3,4-tetrahydronorharman-1-one for the first time within Rubiaceae and ophiorine A and B, two alkaloids with an unusual core bearing a betaine function and a zwitterion as new for the genus. Although the other compounds are already known from other species, their degree of structural diversity highlights the remarkable biosynthetic capabilities of the genus Palicourea. Furthermore, the present paper provides additional support for the hypothesis that tryptamine-iridoid alkaloids represent a distinct chemosystematic feature for the genus Palicourea.
[Mh] Termos MeSH primário: Rubiaceae/química
Triptaminas/química
[Mh] Termos MeSH secundário: Alcaloides/análise
Alcaloides/química
Biodiversidade
Camptotecina
Costa Rica
Iridoides/análise
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Extratos Vegetais/química
Folhas de Planta/química
Alcaloides de Vinca/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Iridoids); 0 (Plant Extracts); 0 (Tryptamines); 0 (Vinca Alkaloids); 0 (strictosamide); 422ZU9N5TV (tryptamine); XT3Z54Z28A (Camptothecin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170815
[St] Status:MEDLINE


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[PMID]:28792865
[Au] Autor:Charles A
[Ad] Endereço:From the UCLA Goldberg Migraine Program, Department of Neurology, David Geffen School of Medicine, University of California, Los Angeles, Los Angeles.
[Ti] Título:Migraine.
[So] Source:N Engl J Med;377(6):553-561, 2017 Aug 10.
[Is] ISSN:1533-4406
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Transtornos de Enxaqueca/terapia
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/uso terapêutico
Antieméticos/uso terapêutico
Peptídeo Relacionado com Gene de Calcitonina/antagonistas & inibidores
Dieta
Feminino
Seres Humanos
Estilo de Vida
Transtornos de Enxaqueca/diagnóstico
Transtornos de Enxaqueca/etiologia
Neurotransmissores/uso terapêutico
Guias de Prática Clínica como Assunto
Triptaminas/uso terapêutico
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antiemetics); 0 (Neurotransmitter Agents); 0 (Tryptamines); 83652-28-2 (Calcitonin Gene-Related Peptide)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170810
[St] Status:MEDLINE
[do] DOI:10.1056/NEJMcp1605502


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[PMID]:28535499
[Au] Autor:Lin W; Huang W; Chen S; Lin M; Huang Q; Huang H
[Ad] Endereço:Department of Neurology, Fujian Medical University Union Hospital, Fuzhou, China.
[Ti] Título:The Role of 5-HTR6 in Mossy Fiber Sprouting: Activating Fyn and p-ERK1/2 in Pilocarpine-Induced Chronic Epileptic Rats.
[So] Source:Cell Physiol Biochem;42(1):231-241, 2017.
[Is] ISSN:1421-9778
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Our primary objective is to verify whether 5-HTR6 is involved in the development of mossy fiber sprouting (MFS), and to determine how the progression of MFS is affected by 5-HTR6. METHODS: A total of 90 male adult Sprague-Dawley rats were allocated into either the control group (n=36) or the epileptic group (n=54). Status epilepticus (SE) of rats was induced by the intraperitoneal (i.p.) injection of LiCl-pilocarpine. We conducted our experiments in two stages. The first stage involves equally dividing 36 epileptic rats into three groups with treatments of none, 5-HTR6 antagonist SB-27104 (SB) and vehicle DMSO. Then behavior and electroencephalogram (EEG) of rats were monitored by video-EEG. The second stage involves dividing 126 epileptic rats into seven groups with treatments of none, 10% DMSO, SB (100 µg/kg), Fyn antagonist PP2 (50 µg/kg), p-ERK1/2 antagonist PD-98059 (30 µg/kg), SB (100 µg/ kg) + PP2 (50 µg/kg); SB (100 µg/kg) + PD-98059 (30 µg/kg). We also treated 18 rats in the control group of the first stage with 100 µg/kg 5-HTR6 agonist WAY-181187 (WAY). MFS of rats was detected through the approach of Timm's staining. Finally, expressions of 5-HTR6, Fyn, p-ERK1/2 and GAP-3 were qualified and semi-quantified via western blotting or RT-PCR. RESULTS: Induction of SE could stimulate formation of MFS and increased GAP-43 expressions. Expressions of 5-HTR6, Fyn and p-ERK1/2 were also up-regulated with increasing time after establishment of SE models. The development of MFS was remarkably inhibited by SB, PP2 and PD. Compared to the single antagonist, such an inhibitory effect was enhanced by SB+PD or SB+PP. Moreover, treatment of healthy rats with WAY would contribute to up-regulated Fyn and p-ERK1/2 expressions, as well as development of MFS (P < 0.05). Suppression of Fyn triggered a down-regulating trend of p-ERK1/2 (P < 0.05), however, suppressed p-ERK1/2 did not have such a significant effect on Fyn expression. CONCLUSION: HTR6 may affect the progression of MFS by activating both p-ERK1/2 and Fyn, which further modulate the expression of GAP-43.
[Mh] Termos MeSH primário: Epilepsia/fisiopatologia
Proteína Quinase 1 Ativada por Mitógeno/metabolismo
Proteína Quinase 3 Ativada por Mitógeno/metabolismo
Proteínas Proto-Oncogênicas c-fyn/metabolismo
Receptores de Serotonina/metabolismo
[Mh] Termos MeSH secundário: Animais
Modelos Animais de Doenças
Epilepsia/induzido quimicamente
Flavonoides/farmacologia
Proteína GAP-43/genética
Proteína GAP-43/metabolismo
Masculino
Proteína Quinase 1 Ativada por Mitógeno/antagonistas & inibidores
Proteína Quinase 3 Ativada por Mitógeno/antagonistas & inibidores
Agonistas Muscarínicos/farmacologia
Pilocarpina/toxicidade
Proteínas Proto-Oncogênicas c-fyn/antagonistas & inibidores
RNA Mensageiro/metabolismo
Ratos
Ratos Sprague-Dawley
Receptores de Serotonina/química
Agonistas de Receptores de Serotonina/farmacologia
Estado Epiléptico/induzido quimicamente
Estado Epiléptico/patologia
Tiazóis/farmacologia
Fatores de Tempo
Triptaminas/farmacologia
Regulação para Cima/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one); 0 (Flavonoids); 0 (GAP-43 Protein); 0 (Muscarinic Agonists); 0 (N(1)-(6-chloroimidazo(2,1-b)(1,3)thiazole-5-sulfonyl)tryptamine); 0 (RNA, Messenger); 0 (Receptors, Serotonin); 0 (Serotonin Receptor Agonists); 0 (Thiazoles); 0 (Tryptamines); 0 (serotonin 6 receptor); 01MI4Q9DI3 (Pilocarpine); EC 2.7.10.2 (Fyn protein, rat); EC 2.7.10.2 (Proto-Oncogene Proteins c-fyn); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 1); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 3)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170713
[Lr] Data última revisão:
170713
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170524
[St] Status:MEDLINE
[do] DOI:10.1159/000477322



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