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Pesquisa : D03.383.129.539 [Categoria DeCS]
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Id: lil-623594
Autor: Marr, J. Joseph; Berens, Randolph L.
Título: Hypoxanthine and inosine analogues as chemotherapeutic agents in chagas' disease
Fonte: Mem. Inst. Oswaldo Cruz;83(supl.1):301-307, Nov. 1988.
Idioma: en.
Conferência: Apresentado em: Annual Meeting on Basic Research in Chagas's disease, 15, Apresentado em: Meeting of the Brazilian Society of Protozoology4, Caxambu, 7-10 Nov. 1988.
Descritores: Doença de Chagas/tratamento farmacológico
Inosina/análogos & derivados
Inosina/uso terapêutico
-Pirazóis/uso terapêutico
Tripanossomicidas
Responsável: BR1.1 - BIREME


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Id: biblio-1016287
Autor: Cardenas, María Paula.
Título: El apixaban se asocia a un menor riesgo de sangrado que los antagonistas de la vitamina K / Apixaban is associated with a lower risk of bleeding than vitamin K antagonists
Fonte: Evid. actual. práct. ambul;21(2):54-54, jul. 2018. tab..
Idioma: es.
Descritores: Pirazóis/efeitos adversos
Piridonas/efeitos adversos
Vitamina K/antagonistas & inibidores
Tromboembolia Venosa/prevenção & controle
Hemorragia/epidemiologia
Anticoagulantes/efeitos adversos
-Pirazóis/uso terapêutico
Piridonas/uso terapêutico
Ensaios Clínicos Controlados Aleatórios como Assunto
Saúde Global
Incidência
Fatores de Risco
Inibidores do Fator Xa/efeitos adversos
Inibidores do Fator Xa/uso terapêutico
Hemorragia/induzido quimicamente
Anticoagulantes/uso terapêutico
Limites: Seres Humanos
Masculino
Feminino
Adulto
Meia-Idade
Idoso
Adulto Jovem
Tipo de Publ: Comentário
Responsável: AR2.1 - Biblioteca Central


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Id: biblio-1011652
Autor: Nusrat, Birjees; Siddiqui, Nadeem; Sahu, Meeta; Naim, Mohd. Javed; Shahar Yar, Mohammad; Ali, Ruhi; Ozair, Alam.
Título: Anticonvulsant evaluation of 2-pyrazolines carrying naphthyl moiety: An insight into synthesis and molecular docking study
Fonte: Braz. j. pharm. sci;55:e00249, 2019. tab, graf, ilus.
Idioma: en.
Resumo: A series of N-substituted-3-(napthalen-2-yl)-5-substituted phenyl-4,5-dihydropyrazole-1-carbothioamide derivatives (4a-n) were synthesized with the view of structural requirements of pharmacophore for potential anticonvulsant agents. The synthesized compounds were assayed intraperitoneally (i.p.) and subcutaneously (s.c.) in mice against seizures induced by MES and scPTZ methods, respectively.Neurologic deficit was evaluated by rotarod method. Among the tested compounds, 4g, 4i, 4j and 4n emerged as the most active molecule in the MES model at a dose of 30 mg/kg at 0.5h comparable to standardscarbamazepine and phenytoin. In the scPTZ test,4e and 4l were found to be most active compounds at the lowest dose of 30 mg/kg at 0.5h, in the management of the convulsive disorder. Molecular docking studies of the titled compounds were also donewith 3D crystal structure of human cytosolic branched chain amino transferase (hBCATc) enzyme and compound 4e was found to have five hydrogen bond interactions with the most important active site residues.In neurotoxicity studies, except compounds 4b, 4c, 4h and 4k, rest of the compounds showed no sign of toxicity.
Descritores: Pirazóis/análise
Anticonvulsivantes/análise
-Epilepsia/diagnóstico
Simulação de Acoplamento Molecular/classificação
Limites: Animais
Masculino
Feminino
Camundongos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-839302
Autor: Chen, B; Hu, N.
Título: Rimonabant improves metabolic parameters partially attributed to restoration of high voltage-activated Ca2+ channels in skeletal muscle in HFD-fed mice
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;50(6):e6141, 2017. graf.
Idioma: en.
Resumo: Cannabinoid type 1 receptor (CB1R) inhibition tends to be one of the promising strategies for the treatment of obesity and other related metabolic disorders. Although CB1R inhibition may cause adverse psychiatric effects including depression and anxiety, the investigation of the role of peripheral CB1R on weight loss and related metabolic parameters are urgently needed. We first explored the effect of rimonabant, a selective CB1R antagonist/inverse agonist, on some metabolic parameters in high fat-diet (HFD)-induced obesity in mice. Then, real-time PCR and electrophysiology were used to explore the contribution of high voltage-activated Ca2+ channels (HVACCs), especially Cav1.1, on rimonabant's effect in skeletal muscle (SM) in HFD-induced obesity. Five-week HFD feeding caused body weight gain, and decreased glucose/insulin tolerance in mice compared to those in the regular diet group (P<0.05), which was restored by rimonabant treatment compared to the HFD group (P<0.05). Interestingly, HVACCs and Cav1.1 were decreased in soleus muscle cells in the HFD group compared to the control group. Daily treatment with rimonabant for 5 weeks was shown to counter such decrease (P<0.05). Collectively, our findings provided a novel understanding for peripheral CB1R's role in the modulation of body weight and glucose homeostasis and highlight peripheral CB1R as well as Cav1.1 in the SM as potential targets for obesity treatment.
Descritores: Glicemia/efeitos dos fármacos
Canais de Cálcio/efeitos dos fármacos
Antagonistas de Receptores de Canabinoides/farmacologia
Músculo Esquelético/efeitos dos fármacos
Piperidinas/farmacologia
Pirazóis/farmacologia
Receptor CB1 de Canabinoide/antagonistas & inibidores
-Peso Corporal/efeitos dos fármacos
Canais de Cálcio Tipo L/efeitos dos fármacos
Canais de Cálcio Tipo L/metabolismo
Canais de Cálcio/metabolismo
Dieta Hiperlipídica/efeitos adversos
Intolerância à Glucose/etiologia
Resistência à Insulina
Camundongos Endogâmicos C57BL
Modelos Animais
Músculo Esquelético/metabolismo
Obesidade/etiologia
Receptor CB1 de Canabinoide/fisiologia
Limites: Animais
Masculino
Responsável: BR1.1 - BIREME


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Id: lil-780891
Autor: Fernandes, Caio Julio Cesar dos Santos; Alves Júnior, José Leonidas; Gavilanes, Francisca; Prada, Luis Felipe; Morinaga, Luciana Kato; Souza, Rogerio.
Título: New anticoagulants for the treatment of venous thromboembolism / Os novos anticoagulantes no tratamento do tromboembolismo venoso
Fonte: J. bras. pneumol;42(2):146-154, Mar.-Apr. 2016. tab, graf.
Idioma: en.
Resumo: Worldwide, venous thromboembolism (VTE) is among the leading causes of death from cardiovascular disease, surpassed only by acute myocardial infarction and stroke. The spectrum of VTE presentations ranges, by degree of severity, from deep vein thrombosis to acute pulmonary thromboembolism. Treatment is based on full anticoagulation of the patients. For many decades, it has been known that anticoagulation directly affects the mortality associated with VTE. Until the beginning of this century, anticoagulant therapy was based on the use of unfractionated or low-molecular-weight heparin and vitamin K antagonists, warfarin in particular. Over the past decades, new classes of anticoagulants have been developed, such as factor Xa inhibitors and direct thrombin inhibitors, which significantly changed the therapeutic arsenal against VTE, due to their efficacy and safety when compared with the conventional treatment. The focus of this review was on evaluating the role of these new anticoagulants in this clinical context.

O tromboembolismo venoso (TEV) está entre as principais causas de morte por doenças cardiovasculares no mundo, atrás apenas do infarto agudo do miocárdio e do acidente vascular cerebral. O TEV possui espectro de apresentação que vai desde a trombose venosa profunda até o tromboembolismo pulmonar agudo, de acordo com gravidade crescente de acometimento, sendo seu tratamento baseado na anticoagulação plena dos pacientes. Há muitas décadas, sabe-se que a anticoagulação interfere diretamente na mortalidade associada ao TEV. Até o início deste século a terapia anticoagulante se baseava no uso de heparina, em suas formas não fracionada ou de baixo peso molecular, e de antagonistas da vitamina K, principalmente a varfarina. Ao longo das últimas décadas, foram desenvolvidos novas classes de medicamentos anticoagulantes, inibidores do fator Xa e inibidores diretos da trombina, que mudaram significativamente o arsenal terapêutico do TEV, em função de suas características de eficácia e segurança em relação ao tratamento convencional, sendo o foco principal de esta revisão avaliar seu papel neste contexto clínico.
Descritores: Anticoagulantes/uso terapêutico
Tromboembolia Venosa/tratamento farmacológico
-Dabigatrana/uso terapêutico
Pirazóis/uso terapêutico
Piridinas/uso terapêutico
Piridonas/uso terapêutico
Rivaroxabana/uso terapêutico
Tiazóis/uso terapêutico
Fatores de Tempo
Varfarina/uso terapêutico
Limites: Seres Humanos
Tipo de Publ: Revisão
Responsável: BR1.1 - BIREME


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Id: lil-751384
Autor: Soares, Wuber J. S.; Lima, Camila A.; Bilton, Tereza L.; Ferrioli, Eduardo; Dias, Rosângela C.; Perracini, Monica R..
Título: Association among measures of mobility-related disability and self-perceived fatigue among older people: a population-based study
Fonte: Braz. j. phys. ther. (Impr.) = Rev. bras. fisioter;19(3):194-200, May-Jun/2015. tab, graf.
Idioma: en.
Projeto: Conselho Nacional de Desenvolvimento Científico e Tecnológico; . FAPEMAT.
Resumo: Objective: To investigate the relationship between self-perceived fatigue with different physical functioning tests and functional performance scales used for evaluating mobility-related disability among community-dwelling older persons. Method: This is a cross-sectional, population-based study. The sample was composed of older persons with 65 years of age or more living in Cuiabá, MT, and Barueri, SP, Brazil. The data for this study is from the FIBRA Network Study. The presence of self-perceived fatigue was assessed using self-reports based on the Center for Epidemiologic Studies-Depression Scale. The Lawton instrumental activities of daily living scale (IADL) and the advanced activities of daily living scale (AADL) were used to assess performance and participation restriction. The following physical functioning tests were used: five-step test (FST), the Short Physical Performance Battery (SPPB), and usual gait speed (UGS). Three models of logistic regression analysis were conducted, and a significance level of α<0.05 was adopted. Results: The sample was composed of 776 older adults with a mean age (SD) of 71.9 (5.9) years, of whom the majority were women (74%). The prevalence of self-perceived fatigue within the participants was 20%. After adjusting for covariates, SPPB, UGS, IADL, and AADL remained associated with self-perceived fatigue in the final multivariate regression model. Conclusion: Our results suggest that there is an association between self-perceived fatigue and lower extremity function, usual gait speed and activity limitation and participation restriction in older adults. Further cohort studies are needed to investigate which physical performance measure may be able to predict the negative impact of fatigue in older adults. .
Descritores: Adenocarcinoma/genética
Carcinoma Pulmonar de Células não Pequenas/genética
Rearranjo Gênico
Neoplasias Pulmonares/genética
Inibidores de Proteínas Quinases/uso terapêutico
Pirazóis/uso terapêutico
Piridinas/uso terapêutico
Receptores Proteína Tirosina Quinases/genética
-Adenocarcinoma/metabolismo
Adenocarcinoma/secundário
Carcinoma Pulmonar de Células não Pequenas/metabolismo
Carcinoma Pulmonar de Células não Pequenas/secundário
Técnicas Imunoenzimáticas
Hibridização in Situ Fluorescente
Neoplasias Pulmonares/metabolismo
Neoplasias Pulmonares/patologia
Prognóstico
Reação em Cadeia da Polimerase em Tempo Real
Reação em Cadeia da Polimerase Via Transcriptase Reversa
RNA Mensageiro/genética
Receptores Proteína Tirosina Quinases/metabolismo
Limites: Adulto
Seres Humanos
Masculino
Tipo de Publ: Relatos de Casos
Responsável: BR1.1 - BIREME


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Id: lil-740321
Autor: Diez-Ewald, María.
Título: Desde el apixaban hasta la aspirina, en la prevención del tromboembolismo venoso recurrente
Fonte: Invest. clín;54(3):231-233, sep. 2013.
Idioma: es.
Descritores: Anticoagulantes/uso terapêutico
Tromboembolia/prevenção & controle
Trombose Venosa/prevenção & controle
-Anticoagulantes/classificação
Anticoagulantes/farmacologia
Antitrombinas/farmacologia
Antitrombinas/uso terapêutico
Aspirina/uso terapêutico
Ensaios Clínicos como Assunto
Inibidores do Fator Xa
Heparina de Baixo Peso Molecular/uso terapêutico
Estudos Multicêntricos como Assunto
Pirazóis/uso terapêutico
Piridonas/uso terapêutico
Recidiva
Trombofilia/tratamento farmacológico
Vitamina K/antagonistas & inibidores
Limites: Seres Humanos
Tipo de Publ: Editorial
Responsável: VE1.1 - Biblioteca Humberto Garcia Arocha


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Id: lil-727667
Autor: Shang, J.L.; Cheng, Q.; Yang, W.F.; Zhang, M.; Cui, Y.; Wang, Y.F..
Título: Possible roles of COX-1 in learning and memory impairment induced by traumatic brain injury in mice
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;47(12):1050-1056, 12/2014. graf.
Idioma: en.
Resumo: People who suffer from traumatic brain injury (TBI) often experience cognitive deficits in spatial reference and working memory. The possible roles of cyclooxygenase-1 (COX-1) in learning and memory impairment in mice with TBI are far from well known. Adult mice subjected to TBI were treated with the COX-1 selective inhibitor SC560. Performance in the open field and on the beam walk was then used to assess motor and behavioral function 1, 3, 7, 14, and 21 days following injury. Acquisition of spatial learning and memory retention was assessed using the Morris water maze on day 15 post-TBI. The expressions of COX-1, prostaglandin E2 (PGE2), interleukin (IL)-6, brain-derived neurotrophic factor (BDNF), platelet-derived growth factor BB (PDGF-BB), synapsin-I, and synaptophysin were detected in TBI mice. Administration of SC560 improved performance of beam walk tasks as well as spatial learning and memory after TBI. SC560 also reduced expressions of inflammatory markers IL-6 and PGE2, and reversed the expressions of COX-1, BDNF, PDGF-BB, synapsin-I, and synaptophysin in TBI mice. The present findings demonstrated that COX-1 might play an important role in cognitive deficits after TBI and that selective COX-1 inhibition should be further investigated as a potential therapeutic approach for TBI.
Descritores: Lesões Encefálicas/complicações
Córtex Cerebral/lesões
Ciclo-Oxigenase 1/fisiologia
Inibidores de Ciclo-Oxigenase/uso terapêutico
Aprendizagem/efeitos dos fármacos
Transtornos da Memória/tratamento farmacológico
Pirazóis/uso terapêutico
-Western Blotting
Fator Neurotrófico Derivado do Encéfalo/metabolismo
Descorticação Cerebral
Ciclo-Oxigenase 1/metabolismo
Modelos Animais de Doenças
Dinoprostona/análise
Dinoprostona/metabolismo
Ensaio de Imunoadsorção Enzimática
Hipocampo/metabolismo
/sangue
INTERLEUKIN-ABDOMEN, ACUTE/sangue
Aprendizagem em Labirinto/efeitos dos fármacos
Transtornos da Memória/etiologia
Transtornos da Memória/metabolismo
MICE, INBRED CABDOMENABDOMINAL INJURIESBL
Proteínas Proto-Oncogênicas c-sis/metabolismo
Recuperação de Função Fisiológica/efeitos dos fármacos
Sinaptofisina/análise
Sinaptofisina/metabolismo
Limites: Animais
Responsável: BR1.1 - BIREME


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Id: lil-723170
Autor: Nascimento, Carla Lessa Pena; Garcia, Cecilia Lopes; Schvartsman, Benita Galassi Soares; Vaisbich, Maria Helena.
Título: Treatment of Bartter syndrome. Unsolved issue, / Tratamento da síndrome de Bartter. Problema não resolvido,
Fonte: J. pediatr. (Rio J.);90(5):512-517, Sep-Oct/2014. tab, graf.
Idioma: en.
Resumo: Objective: To describe the results of a long-term follow-up of Bartter syndrome patients treated with different drugs. Method: Patients were diagnosed according to clinical and laboratory data. Treatment protocol was potassium supplementation, sodium, spironolactone, and non-steroidal anti-inflammatory drug. Patients who developed proteinuria were converted to angiotensin conversion enzyme inhibitor. The variables evaluated for each drug were Z-score for weight and stature, proteinuria, creatinine clearance, gastrointestinal complaints, amount of potassium supplementation, serum potassium and bicarbonate levels, and findings of upper digestive endoscopy. Results: 20 patients were included. Follow-up was 10.1 ± 5.2 years. 17 patients received indomethacin for 5.9 ± 5.3 years; 19 received celecoxib, median of 35 months; and five received enalapril, median of 23 months. During indomethacin, a statistically significant increase was observed in the Z-score for stature and weight, without a change in the creatinine clearance. Seven of 17 patients had gastrointestinal symptoms, and upper digestive endoscopy evidenced gastritis in three patients and gastric ulcer in four patients. During celecoxib use, a significant increase was detected in the Z-score for stature and weight and a reduction of hyperfiltration; seven patients presented gastrointestinal symptoms, and upper digestive endoscopy evidenced mild gastritis in three. During enalapril use, no significant changes were observed in the Z-score for stature, weight and creatinine clearance. The conversion to enalapril resulted in a significant reduction in proteinuria. Conclusion: The authors suggest starting the treatment with celecoxib, and replacing by ACEi if necessary, monitoring the renal function. The safety and efficacy of celecoxib need to be assessed in larger controlled studies. .

Objetivo: Descrever os resultados de um acompanhamento de longo prazo de pacientes com síndrome de Bartter tratados com diferentes medicamentos. Método: Pacientes diagnosticados segundo os dados clínicos e laboratoriais. Protocolo de tratamento: suplementação de potássio, sódio, espironolactona e medicamento anti-inflamatório não esteroidal. Os pacientes que desenvolveram proteinúria foram submetidos a inibidor da enzima de conversão da angiotensina. As variáveis avaliadas durante o uso de cada medicamento foram: escore Z para peso e estatura, proteinúria, depuração da creatinina, queixas gastrointestinais, quantidade da suplementação de potássio, níveis séricos de potássio e bicarbonato e achados da endoscopia digestiva alta. Resultados: Foram incluídos 20 pacientes. O acompanhamento foi de 10,1 ± 5,2 anos. No total, 17 pacientes receberam indometacina por 5,9 ± 5,3 anos, 19 receberam celecoxib por aproximadamente 35 meses e cinco receberam enalapril por aproximadamente 23 meses. Durante o uso de indometacina, observamos um aumento estatístico significativo no escore Z para estatura e peso, sem alteração na depuração da creatinina. 7/17 pacientes apresentaram sintomas gastrointestinais, e a endoscopia digestiva alta mostrou gastrite em três pacientes e úlcera gástrica em quatro. Durante o uso de celecoxib, detectamos um aumento significativo no escore Z para estatura e peso e uma redução da hiperfiltração; sete pacientes apresentaram sintomas gastrointestinais e a endoscopia digestiva alta mostrou gastrite leve em três pacientes. Durante o uso de enalapril, não observamos alterações significativas no escore Z para estatura, peso e depuração da creatinina. A mudança da medicação para enalapril resultou em uma ...
Descritores: Síndrome de Bartter/tratamento farmacológico
Inibidores de Ciclo-Oxigenase/uso terapêutico
Enalapril/uso terapêutico
Indometacina/uso terapêutico
Pirazóis/uso terapêutico
Sulfonamidas/uso terapêutico
-Síndrome de Bartter/complicações
Bicarbonatos/sangue
Estatura/efeitos dos fármacos
Peso Corporal/efeitos dos fármacos
Creatinina/análise
Seguimentos
Potássio/sangue
Proteinúria/tratamento farmacológico
Proteinúria/etiologia
Estudos Retrospectivos
Fatores de Tempo
Resultado do Tratamento
Limites: Feminino
Seres Humanos
Lactente
Masculino
Responsável: BR1.1 - BIREME


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Id: lil-714578
Autor: Dornelas, Conceição Aparecida; Cavalcanti, Bruno Coelho; Magalhães, Hemerson Iury Ferreira; Jamacaru, Francisco Vagnaldo Fechine; Furtado, Francisco Nelson Nóbrega; Juanes, Camila de Carvalho; Melo, Nayanna de Oliveira Ramos; Moraes, Manoel Odorico de.
Título: Potential chemoprotective effects of green propolis, L-lysine and celecoxib on bone marrow cells and peripheral blood lymphocytes of Wistar rats subjected to bladder chemical carcinogenesis
Fonte: Acta cir. bras;29(7):423-428, 07/2014. tab, graf.
Idioma: en.
Resumo: PURPOSE: To evaluate the genotoxicity of propolis and L-lysine, as well as their effects on the possible cellular damage in erythroblasts (bone marrow) and leukocytes (peripheral blood) caused by the carcinogen BBN (n - butyl - n {4 - hydroxybutyl} nitrosamine) in rats subjected to bladder carcinogenesis and treated with green propolis and L-lysine. METHODS: One hundred and twenty five rats were distributed into the following groups: I, IIA, IIB, III, K, L M N, X, XI, XII and XIII. Groups I to X received BBN in drinking water for 14 weeks (wks). Group I was treated with intragastric (ig) propolis at 150 mg/kg body weight, for 44 wks, beginning 30 days before start of BBN. Groups IIA and III were treated with propolis (150 mg/kg), for 40 wks, subcutaneous (sc) and ig, respectively, beginning simultaneously with BBN. On the 32nd wk, the animals of groups L, M and N were treated ig with L-lysine (300 mg/kg), celecoxib (30 mg/kg) and propolis (300 mg/kg), respectively, up to the 40th wk. The groups that received only BBN (IIB and K) were treated with water, sc and orally, respectively, for 40 wks. Groups XI, XII and XIII received respectively propolis (150 mg/kg), L-lysine (150 mg/kg) and water ig for 40 wks. After 40 wks, the surviving animals were anesthetized and subjected to femoral bone marrow aspiration and blood collection from the aorta, for CA and MNT, respectively, for investigation of genotoxicity. RESULTS: Groups IIB and K, which received only BBN and water, showed the greatest DNA damage in peripheral leukocytes (CA) and largest number of micronuclei in bone marrow erythrocytes (MNT) in relation to all other groups that received BBN and lysine and/or propolis (p<0.001). CONCLUSIONS: Both propolis and L-lysine are effective in protecting against genotoxicity, as well not being genotoxic themselves toward the cells evaluated, at the doses and times administered and according to the two tests utilized. .
Descritores: Células da Medula Óssea/efeitos dos fármacos
Carcinogênese/efeitos dos fármacos
Linfócitos/efeitos dos fármacos
Lisina/farmacologia
Própole/farmacologia
Pirazóis/farmacologia
Sulfonamidas/farmacologia
-Anticarcinógenos/farmacologia
Testes de Carcinogenicidade
Ensaio Cometa
Dano ao DNA
Testes para Micronúcleos
Ratos Wistar
Valores de Referência
Reprodutibilidade dos Testes
Fatores de Tempo
Neoplasias da Bexiga Urinária/patologia
Neoplasias da Bexiga Urinária/prevenção & controle
Limites: Animais
Tipo de Publ: Estudos de Avaliação
Responsável: BR1.1 - BIREME



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