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[PMID]:29427588
[Au] Autor:Nishimura-Danjobara Y; Oyama K; Yokoigawa K; Oyama Y
[Ad] Endereço:Department of Food Science, Faculty of Bioscience and Bioindustry, Tokushima University, Tokushima 770-8513, Japan.
[Ti] Título:Hyperpolarization by N-(3-oxododecanoyl)-l-homoserine-lactone, a quorum sensing molecule, in rat thymic lymphocytes.
[So] Source:Chem Biol Interact;283:91-96, 2018 Mar 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:To study the adverse effects of N-(3-oxododecanoyl)-l-homoserine-lactone (ODHL), a quorum sensing molecule, on mammalian host cells, its effect on membrane potential was examined in rat thymic lymphocytes using flow cytometric techniques with a voltage-sensitive fluorescent probe. As 3-300 µM ODHL elicited hyperpolarization, it is likely that it increases membrane K permeability because hyperpolarization is directly linked to changing K gradient across membranes, but not Na and Cl gradients. ODHL did not increase intracellular Ca concentration. ODHL also produced a response in the presence of an intracellular Zn chelator. Thus, it is unlikely that intracellular Ca and Zn are attributed to the response. Quinine, a non-specific K channel blocker, greatly reduced hyperpolarization. However, because charybdotoxin, tetraethylammonium chloride, 4-aminopyridine, and glibenclamide did not affect it, it is pharmacologically hypothesized that Ca -activated K channels, voltage-gated K channels, and ATP-sensitive K channels are not involved in ODHL-induced hyperpolarization. Although the K channels responsible for ODHL-induced hyperpolarization have not been identified, it is suggested that ODHL can elicit hyperpolarization in mammalian host cells, disturbing cellular functions.
[Mh] Termos MeSH primário: 4-Butirolactona/análogos & derivados
Polaridade Celular/efeitos dos fármacos
Homosserina/análogos & derivados
Percepção de Quorum/efeitos dos fármacos
[Mh] Termos MeSH secundário: 4-Butirolactona/farmacologia
Animais
Cálcio/metabolismo
Charibdotoxina/farmacologia
Citometria de Fluxo
Glibureto/farmacologia
Homosserina/farmacologia
Canais KATP/metabolismo
Linfócitos/citologia
Linfócitos/efeitos dos fármacos
Linfócitos/metabolismo
Permeabilidade/efeitos dos fármacos
Potássio/metabolismo
Canais de Potássio de Abertura Dependente da Tensão da Membrana/metabolismo
Quinina/farmacologia
Ratos
Ratos Wistar
Timócitos/citologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (KATP Channels); 0 (N-(3-oxododecanoyl)homoserine lactone); 0 (Potassium Channels, Voltage-Gated); 115422-61-2 (Charybdotoxin); 6KA95X0IVO (Homoserine); A7V27PHC7A (Quinine); OL659KIY4X (4-Butyrolactone); RWP5GA015D (Potassium); SX6K58TVWC (Glyburide); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180211
[St] Status:MEDLINE


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[PMID]:29419672
[Au] Autor:Alemi H; Khaloo P; Mansournia MA; Rabizadeh S; Salehi SS; Mirmiranpour H; Meftah N; Esteghamati A; Nakhjavani M
[Ad] Endereço:Endocrinology and Metabolism Research Center (EMRC), Vali-Asr Hospital, School of Medicine.
[Ti] Título:Pulse pressure and diabetes treatments: Blood pressure and pulse pressure difference among glucose lowering modality groups in type 2 diabetes.
[So] Source:Medicine (Baltimore);97(6):e9791, 2018 Feb.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Type 2 diabetes is associated with higher pulse pressure. In this study, we assessed and compared effects of classic diabetes treatments on pulse pressure (PP), systolic blood pressure (SBP), and diastolic blood pressure (DBP) in patients with type 2 diabetes.In a retrospective cohort study, 718 non-hypertensive patients with type 2 diabetes were selected and divided into 4 groups including metformin, insulin, glibenclamide+metformin, and metformin+insulin. They were followed for 4 consecutive visits lasting about 45.5 months. Effects of drug regimens on pulse and blood pressure over time were assessed separately and compared in regression models with generalized estimating equation method and were adjusted for age, duration of diabetes, sex, smoking, and body mass index (BMI).Studied groups had no significant change in PP, SBP, and DBP over time. No significant difference in PP and DBP among studied groups was observed (PP:P = 0.090; DBP:P = 0.063). Pairwise comparisons of PP, SBP, and DBP showed no statistically significant contrast between any 2 studied groups. Interactions of time and treatment were not different among groups.Our results demonstrate patients using metformin got higher PP and SBP over time. Averagely, pulse and blood pressure among groups were not different. Trends of variation in pulse and blood pressure were not different among studied diabetes treatments.
[Mh] Termos MeSH primário: Pressão Sanguínea
Diabetes Mellitus Tipo 2
Glucose/análise
Glibureto/administração & dosagem
Insulina/administração & dosagem
Metformina/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Pressão Sanguínea/efeitos dos fármacos
Pressão Sanguínea/fisiologia
Determinação da Pressão Arterial/métodos
Estudos de Coortes
Diabetes Mellitus Tipo 2/diagnóstico
Diabetes Mellitus Tipo 2/tratamento farmacológico
Diabetes Mellitus Tipo 2/epidemiologia
Diabetes Mellitus Tipo 2/fisiopatologia
Quimioterapia Combinada/métodos
Feminino
Seres Humanos
Hipoglicemiantes/administração & dosagem
Irã (Geográfico)/epidemiologia
Masculino
Meia-Idade
Avaliação de Processos e Resultados (Cuidados de Saúde)
Estudos Retrospectivos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (Insulin); 9100L32L2N (Metformin); IY9XDZ35W2 (Glucose); SX6K58TVWC (Glyburide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:180209
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000009791


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[PMID]:29224994
[Au] Autor:Kuang Y; Li B; Fan J; Qiao X; Ye M
[Ad] Endereço:State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing 100191, China.
[Ti] Título:Antitussive and expectorant activities of licorice and its major compounds.
[So] Source:Bioorg Med Chem;26(1):278-284, 2018 01 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Licorice has been used as an antitussive and expectorant herbal medicine for a long history. This work evaluated the activities of 14 major compounds and crude extracts of licorice, using the classical ammonia-induced cough model and phenol red secretion model in mice. Liquiritin apioside (1), liquiritin (2), and liquiritigenin (3) at 50 mg/kg (i.g.) could significantly decrease cough frequency by 30-78% (p < .01). The antitussive effects could be partially antagonized by the pretreatment of methysergide or glibenclamide, but not naloxone. Moreover, compounds 1-3 showed potent expectorant activities after 3 days treatment (p < .05). The water and ethanol extracts of licorice, which contain abundant 1 and 2, could decrease cough frequency at 200 mg/kg by 25-59% (p < .05), and enhance the phenol red secretion (p < .05), while the ethyl acetate extract showed little effect. These results indicate liquiritin apioside and liquiritin are the major antitussive and expectorant compounds of licorice. Their antitussive effects depend on both peripheral and central mechanisms.
[Mh] Termos MeSH primário: Antitussígenos/farmacologia
Tosse/tratamento farmacológico
Expectorantes/farmacologia
Glycyrrhiza/química
Fenolsulfonaftaleína/metabolismo
Extratos Vegetais/farmacologia
[Mh] Termos MeSH secundário: Administração Oral
Amônia
Animais
Antitussígenos/antagonistas & inibidores
Antitussígenos/química
Tosse/induzido quimicamente
Modelos Animais de Doenças
Relação Dose-Resposta a Droga
Expectorantes/química
Expectorantes/isolamento & purificação
Glibureto/farmacologia
Masculino
Metisergida/farmacologia
Camundongos
Camundongos Endogâmicos ICR
Estrutura Molecular
Extratos Vegetais/química
Extratos Vegetais/isolamento & purificação
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antitussive Agents); 0 (Expectorants); 0 (Plant Extracts); 7664-41-7 (Ammonia); I6G9Y0J1OJ (Phenolsulfonphthalein); SX6K58TVWC (Glyburide); XZA9HY6Z98 (Methysergide)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180106
[Lr] Data última revisão:
180106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE


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[PMID]:29190739
[Au] Autor:Loos JA; Churio MS; Cumino AC
[Ad] Endereço:Laboratorio de Zoonosis Parasitarias, Departamento de Biología, Facultad de Ciencias Exactas y Naturales, Universidad Nacional de Mar del Plata (UNMdP), Mar del Plata, Argentina.
[Ti] Título:Anthelminthic activity of glibenclamide on secondary cystic echinococcosis in mice.
[So] Source:PLoS Negl Trop Dis;11(11):e0006111, 2017 Nov.
[Is] ISSN:1935-2735
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cystic echinococcosis (CE) is a worldwide parasitic zoonosis caused by the larval stage of Echinococcus granulosus. Current chemotherapy against this disease is based on the administration of benzimidazoles (BZMs). However, BZM treatment has a low cure rate and causes several side effects. Therefore, new treatment options are needed. The antidiabetic drug glibenclamide (Glb) is a second-generation sulfonylurea receptor inhibitor that has been shown to be active against protozoan parasites. Hence, we assessed the in vitro and in vivo pharmacological effects of Glb against the larval stage of E. granulosus. The in vitro activity was concentration dependent on both protoscoleces and metacestodes. Moreover, Glb combined with the minimum effective concentration of albendazole sulfoxide (ABZSO) was demonstrated to have a greater effect on metacestodes in comparison with each drug alone. Likewise, there was a reduction in the cyst weight after oral administration of Glb to infected mice (5 mg/kg of body weight administered daily for a period of 8 weeks). However, in contrast to in vitro assays, no differences in effectiveness were found between Glb + albendazole (ABZ) combined treatment and Glb monotherapy. Our results also revealed mitochondrial membrane depolarization and an increase in intracellular Ca2+ levels in Glb-treated protoscoleces. In addition, the intracystic drug accumulation and our bioinformatic analysis using the available E. granulosus genome suggest the presence of genes encoding sulfonylurea transporters in the parasite. Our data clearly demonstrated an anti-echinococcal effect of Glb on E. granulosus larval stage. Further studies are needed in order to thoroughly investigate the mechanism involved in the therapeutic response of the parasite to this sulfonylurea.
[Mh] Termos MeSH primário: Anti-Helmínticos/administração & dosagem
Equinococose/tratamento farmacológico
Echinococcus granulosus/efeitos dos fármacos
Glibureto/administração & dosagem
Hipoglicemiantes/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oral
Animais
Anti-Helmínticos/farmacologia
Modelos Animais de Doenças
Equinococose/patologia
Glibureto/farmacologia
Camundongos
Testes de Sensibilidade Parasitária
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Hypoglycemic Agents); SX6K58TVWC (Glyburide)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171229
[Lr] Data última revisão:
171229
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171201
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pntd.0006111


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[PMID]:28961497
[Au] Autor:Peng J; Deng X; Huang W; Yu JH; Wang JX; Wang JP; Yang SB; Liu X; Wang L; Zhang Y; Zhou XY; Yang H; He YZ; Xu FY
[Ad] Endereço:Department of Rehabilitation, Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, 646000, PR China.
[Ti] Título:Irisin protects against neuronal injury induced by oxygen-glucose deprivation in part depends on the inhibition of ROS-NLRP3 inflammatory signaling pathway.
[So] Source:Mol Immunol;91:185-194, 2017 11.
[Is] ISSN:1872-9142
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Recent studies found that irisin, a newly discovered skeletal muscle-derived myokine during exercise, is also synthesized in various tissues of different species and protects against neuronal injury in cerebral ischemia. The NOD-like receptor pyrin 3 (NLRP3) inflammasome play an important role in detecting cellular damage and mediating inflammatory responses to aseptic tissue injury during ischemic stroke. However, it is unclear whether irisin is involved in the regulation of NLRP3 inflammasome activation during ischemic stroke. In the present study, PC12 neuronal cells were exposed to oxygen-glucose deprivation (OGD), exogenous irisin (12.5, 25, 50nmol/L) or NLRP3 inhibitor glyburide (50, 100, 200µmol/L) were used as an intervention reagent, NLRP3 was over-expressed or suppressed by transfection with a NLRP3 expressing vector or NLRP3-specifc siRNA, respectively. Our data showed that both irisin and its precursor protein fibronectin type III domain containing 5 (FNDC5) expression were significantly down-regulated (p<0.05); but oxidative stress and ROS-NLRP3 inflammasome signaling were activated by OGD (p<0.05); treatment with irisin or inhibition of NLRP3 reversed OGD-induced oxidative stress and inflammation (p<0.05). However, these irisin-mediated effects were blunted by over-expression NLRP3 (p<0.05). Taken together, our results firstly revealed that irisin mitigated OGD-induced neuronal injury in part via inhibiting ROS-NLRP3 inflammatory signaling pathway, suggesting a likely mechanism for irisin-induced therapeutic effect in ischemic stroke.
[Mh] Termos MeSH primário: Fibronectinas/imunologia
Glucose/imunologia
Proteína 3 que Contém Domínio de Pirina da Família NLR/imunologia
Neurônios/imunologia
Oxigênio/imunologia
Espécies Reativas de Oxigênio/imunologia
Transdução de Sinais/imunologia
[Mh] Termos MeSH secundário: Animais
Isquemia Encefálica/imunologia
Isquemia Encefálica/metabolismo
Isquemia Encefálica/patologia
Fibronectinas/metabolismo
Glucose/metabolismo
Glibureto/farmacologia
Células HeLa
Seres Humanos
Inflamação/imunologia
Inflamação/metabolismo
Inflamação/patologia
Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo
Neurônios/metabolismo
Neurônios/patologia
Oxigênio/metabolismo
Células PC12
Ratos
Espécies Reativas de Oxigênio/metabolismo
Transdução de Sinais/efeitos dos fármacos
Acidente Vascular Cerebral/imunologia
Acidente Vascular Cerebral/metabolismo
Acidente Vascular Cerebral/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (FNDC5 protein, human); 0 (FNDC5 protein, rat); 0 (Fibronectins); 0 (NLR Family, Pyrin Domain-Containing 3 Protein); 0 (NLRP3 protein, human); 0 (Nlrp3 protein, rat); 0 (Reactive Oxygen Species); IY9XDZ35W2 (Glucose); S88TT14065 (Oxygen); SX6K58TVWC (Glyburide)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171120
[Lr] Data última revisão:
171120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170930
[St] Status:MEDLINE


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[PMID]:28930827
[Au] Autor:Liang HL; Ma SJ; Xiao YN; Tan HZ
[Ad] Endereço:Department of Epidemiology and Statistics, Xiangya School of Public Health, Central South University, Changsha, Hunan, China.
[Ti] Título:Comparative efficacy and safety of oral antidiabetic drugs and insulin in treating gestational diabetes mellitus: An updated PRISMA-compliant network meta-analysis.
[So] Source:Medicine (Baltimore);96(38):e7939, 2017 Sep.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The safety and efficacy of different drugs in treatment of gestational diabetes mellitus (GDM) patients who could not maintain normal glucose level only through diet and exercise remains to be debated. We performed this network meta-analysis (NAM) to compare and rank different antidiabetic drugs in glucose level control and pregnancy outcomes in GDM patients. METHODS: We searched PubMed, Cochrane Library, Web of Science, and Embase up to December 31, 2016. Randomized controlled trials (RCTs) related to different drugs in the treatment of GDM patients were enrolled. We extracted the relevant information and assessed the risk of bias with the Cochrane risk of bias tool. We did pair-wise meta-analyses using the fixed-effects model or random-effects model and then adopted random-effects NAM combining both direct and indirect evidence within a Bayesian framework, to calculate the odds ratio (OR) or standardized mean difference (SMD) and to draw a surface under the cumulative ranking curve of the neonatal and maternal outcomes of different treatments in GDM patients. RESULTS: Thirty-two randomized controlled trials (RCTs) were included in this NAM, including 6 kinds of treatments (metformin, metformin plus insulin, insulin, glyburide, acarbose, and placebo). The results of the NAM showed that regarding the incidence of macrosomia and LGA, metformin had lower incidence than glyburide (OR, 0.5411 and 0.4177). In terms of the incidence of admission to the NICU, insulin had higher incidence compared with glyburide (OR, 1.844). As for the incidence of neonatal hypoglycemia, metformin had lower incidence than insulin and glyburide (OR, 0.6331 and 0.3898), and insulin was lower than glyburide (OR, 0.6236). For mean birth weight, metformin plus insulin was lower than insulin (SMD, -0.5806), glyburide (SMD, -0.7388), and placebo (SMD, -0.6649). Besides, metformin was observed to have lower birth weight than glyburide (SMD, 0.2591). As for weight gain, metformin and metformin plus insulin were lower than insulin (SMD, -0.9166, -1.53). Ranking results showed that glyburide might be the optimum treatment regarding average glucose control, and metformin is the fastest in glucose control for GDM patients; glyburide have the highest incidence of macrosomia, preeclampsia, hyperbilirubinemia, neonatal hypoglycemia, shortest gestational age at delivery, and lowest mean birth weight; metformin (plus insulin when required) have the lowest incidence of macrosomia, PIH, LGA, RDS, low gestational age at delivery, and low birth weight. Besides, insulin had the highest incidence of NICU admission, acarbose had the lowest risk of neonatal hypoglycemia. CONCLUSION: Our study concluded that metformin is fastest in glucose control, with a more favorable pregnancy outcomes-would be a better option, but its rate of glucose control is the lowest.However, glyburide is the optimumtreatment regarding the rate of glucose control, but withmore adverse outcomes. This NAMbased on 32 RCTs will strongly help to guide further development of management for GDM patients, clinicians should carefully balance the risk-benefit profile of different treatments according to various situations.
[Mh] Termos MeSH primário: Diabetes Gestacional/tratamento farmacológico
Glibureto/administração & dosagem
Hipoglicemiantes/administração & dosagem
Insulina/administração & dosagem
Metformina/administração & dosagem
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Glicemia/efeitos dos fármacos
Pesquisa Comparativa da Efetividade
Diabetes Gestacional/sangue
Feminino
Macrossomia Fetal/induzido quimicamente
Macrossomia Fetal/epidemiologia
Glibureto/efeitos adversos
Seres Humanos
Hipoglicemiantes/efeitos adversos
Incidência
Recém-Nascido
Insulina/efeitos adversos
Metformina/efeitos adversos
Gravidez
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS
[Nm] Nome de substância:
0 (Blood Glucose); 0 (Hypoglycemic Agents); 0 (Insulin); 9100L32L2N (Metformin); SX6K58TVWC (Glyburide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171015
[Lr] Data última revisão:
171015
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170921
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000007939


  7 / 5935 MEDLINE  
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[PMID]:28918294
[Au] Autor:Abd Elmoneim H; Sharabi F; Mohy El Din M; Louedec L; Norel X; Senbel A
[Ad] Endereço:Department of Pharmacology and Toxicology, Faculty of Pharmacy, Alexandria University, Egypt.
[Ti] Título:Potassium channels modulate the action but not the synthesis of hydrogen sulfide in rat corpus cavernosum.
[So] Source:Life Sci;189:39-43, 2017 Nov 15.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIM: Hydrogen sulfide (H S) is a newly-introduced gasotransmitter in penile tissues. However, its exact mechanism of action in mediating penile erection is not fully elucidated. The major aim of this study was to examine the role of different K channels in mediating the responses to H S in the corpus cavernosum. MAIN METHODS: Tension studies using isolated rat corpus cavernosum strips were conducted. Endogenous H S production was measured using polarographic technique. Results are expressed as mean±SEM. KEY FINDINGS: l-Cysteine (10 M) stimulated rat corpus cavernosum to produce H S. Blockade of CSE by BCA (10 M) reduced the concentration of H S produced from rat corpus cavernosum significantly. Addition of TEA (10 M) or 4-AP (10 M) didn't have a significant effect on the concentration of H S produced. l-Cysteine (10 -10 M) elicited a concentration-dependent relaxation response which was significantly reduced by blockade of CSE using BCA (10 M). TEA (10 M), 4-AP (10 M) and TEA (10 M) attenuated l-cysteine-induced relaxation significantly. At 10 M, l-cysteine resulted in percentage relaxation of 1.55±0.63, 10.94±1.93 and 1.93±0.80 in presence of TEA (10 M), 4-AP (10 M) and TEA (10 M) respectively compared to 23.78±2.71 as control. Both glibenclamide (10 M) and BaCl (3×10 M) failed to reduce these relaxations significantly. SIGNIFICANCE: H S-induced relaxation of rat corpus cavernosum may be mediated - at least in part - through BK and K channels not by K and K channels. It also seems that K -channels do not contribute to the synthesis of H S.
[Mh] Termos MeSH primário: Sulfeto de Hidrogênio/metabolismo
Pênis/metabolismo
Canais de Potássio/metabolismo
[Mh] Termos MeSH secundário: Alanina/administração & dosagem
Alanina/análogos & derivados
Alanina/farmacologia
Animais
Cisteína/administração & dosagem
Cisteína/farmacologia
Relação Dose-Resposta a Droga
Glibureto/farmacologia
Masculino
Ratos
Ratos Wistar
Tetraetilamônio/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Potassium Channels); 66-40-0 (Tetraethylammonium); 923-01-3 (3-cyanoalanine); K848JZ4886 (Cysteine); OF5P57N2ZX (Alanine); SX6K58TVWC (Glyburide); YY9FVM7NSN (Hydrogen Sulfide)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170918
[St] Status:MEDLINE


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[PMID]:28855109
[Au] Autor:Li H; Kim HW; Shin SE; Seo MS; An JR; Ha KS; Han ET; Hong SH; Firth AL; Choi IW; Han IY; Lee DS; Yim MJ; Park WS
[Ad] Endereço:Department of Physiology, Kangwon National University School of Medicine, Chuncheon 24341, South Korea.
[Ti] Título:The vasorelaxant effect of mitiglinide via activation of voltage-dependent K channels and SERCA pump in aortic smooth muscle.
[So] Source:Life Sci;188:1-9, 2017 Nov 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: The vasorelaxant effects of the anti-diabetic drug, mitiglinide in phenylephrine (Phe)-pre-contracted aortic rings were examined. MATERIALS AND METHODS: Arterial tone measurement was performed in aortic smooth muscle cells. KEY FINDINGS: Mitiglinide dose-dependently induced vasorelaxation. Application of the large-conductance Ca -activated K (BK ) channel blocker paxilline, inwardly rectifying K (Kir) channel blocker Ba , and ATP-sensitive K (K ) channel blocker glibenclamide did not affect the vasorelaxant effect of mitiglinide. However, application of the voltage-dependent K (Kv) channel blocker 4-AP, effectively inhibited mitiglinide-induced vasorelaxation. Although pretreatment with the Ca channel blocker nifedipine did not alter the mitiglinide-induced vasorelaxation, pretreatment with the sarcoplasmic/endoplasmic reticulum Ca -ATPase (SERCA) pump inhibitor thapsigargin and cyclopiazonic acid reduced the vasorelaxant effect of mitiglinide. In addition, the vasorelaxant effect of mitiglinide was not affected by the inhibitors of adenylyl cyclase, protein kinase A, guanylyl cyclase, or protein kinase G. Elimination of the endothelium and inhibition of endothelium-dependent vasorelaxant mechanisms also did not change the vasorelaxant effect of mitiglinide. SIGNIFICANCE: We proposed that mitiglinide induces vasorelaxation via activation of Kv channels and SERCA pump. However, the vasorelaxant effects of mitiglinide did not involve other K channels, Ca channels, PKA/PKG signaling pathways, or the endothelium.
[Mh] Termos MeSH primário: Aorta Torácica/fisiologia
Isoindóis/farmacologia
Músculo Liso/fisiologia
Canais de Potássio de Abertura Dependente da Tensão da Membrana/agonistas
ATPases Transportadoras de Cálcio do Retículo Sarcoplasmático/fisiologia
Vasodilatadores/farmacologia
[Mh] Termos MeSH secundário: 4-Aminopiridina/farmacologia
Adenina/análogos & derivados
Adenina/farmacologia
Animais
Aorta Torácica/efeitos dos fármacos
Bário/farmacologia
Carbazóis/farmacologia
Relação Dose-Resposta a Droga
Interações Medicamentosas
Endotélio Vascular/efeitos dos fármacos
Glibureto/farmacologia
Indóis/farmacologia
Isoindóis/antagonistas & inibidores
Masculino
Músculo Liso/efeitos dos fármacos
Nifedipino/farmacologia
Oxidiazóis/farmacologia
Fenilefrina/farmacologia
Pirróis/farmacologia
Quinoxalinas/farmacologia
Coelhos
ATPases Transportadoras de Cálcio do Retículo Sarcoplasmático/antagonistas & inibidores
Transdução de Sinais/efeitos dos fármacos
Tapsigargina/farmacologia
Vasodilatadores/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one); 0 (Carbazoles); 0 (Indoles); 0 (Isoindoles); 0 (Oxadiazoles); 0 (Potassium Channels, Voltage-Gated); 0 (Pyrroles); 0 (Quinoxalines); 0 (Vasodilator Agents); 126643-37-6 (KT 5823); 17318-31-9 (9-(tetrahydro-2-furyl)-adenine); 1WS297W6MV (Phenylephrine); 24GP945V5T (Barium); 3T9U9Z96L7 (paxilline); 58HV29I28S (KT 5720); 67526-95-8 (Thapsigargin); BH3B64OKL9 (4-Aminopyridine); D86I0XLB13 (mitiglinide); EC 3.6.3.8 (Sarcoplasmic Reticulum Calcium-Transporting ATPases); I9ZF7L6G2L (Nifedipine); JAC85A2161 (Adenine); SX6K58TVWC (Glyburide); X9TLY4580Z (cyclopiazonic acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE


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[PMID]:28847172
[Au] Autor:Hedrington MS; Davis SN
[Ad] Endereço:a Department of Medicine , University of Maryland School of Medicine , Baltimore , MD , USA.
[Ti] Título:The care of pregestational and gestational diabetes and drug metabolism considerations.
[So] Source:Expert Opin Drug Metab Toxicol;13(10):1029-1038, 2017 Oct.
[Is] ISSN:1744-7607
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Normal pregnancy development involves gradual decline in insulin sensitivity, which sometimes requires pharmacotherapy. Insulin is the drug of choice for gestational and pregestational diabetes. Metabolism of traditional insulins results in inadequate onset and duration of action and marked peak activity. These properties increase risk of excessive glucose excursions, which are especially undesirable during pregnancy. Insulin analogs have been emerging as a safer and more effective treatment of diabetes during pregnancy. Areas covered: This manuscript reviews currently used antihyperglycemic agents: fast and long-acting insulins, metformin and glyburide. Trials demonstrating their efficacy and safety during pregnancy are described. Certain drug metabolism considerations (e.g. affinity to IGF-1) are emphasized. Expert opinion: The theories that insulin analogs bind to immunoglobulin and cross placenta have been disproved. Lispro, aspart, glargine and detemir do not transfer across the placenta and do not result in adverse maternal and neonatal outcomes. In addition, favorable pharmacokinetic profiles (rapid onset and 24-hour near peakless activity) substantially reduce blood glucose variability including hypoglycemia. We believe that insulin analogs should be given strong consideration for the treatment of diabetes during pregnancy. Metformin has also proven to be safe and may be considered as an initial single agent for milder gestational diabetes.
[Mh] Termos MeSH primário: Diabetes Gestacional/tratamento farmacológico
Hipoglicemiantes/administração & dosagem
Gravidez em Diabéticas/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Glicemia/efeitos dos fármacos
Feminino
Glibureto/administração & dosagem
Glibureto/efeitos adversos
Glibureto/farmacocinética
Seres Humanos
Hipoglicemia/induzido quimicamente
Hipoglicemiantes/efeitos adversos
Hipoglicemiantes/farmacocinética
Insulina/administração & dosagem
Insulina/efeitos adversos
Insulina/farmacocinética
Metformina/administração & dosagem
Metformina/efeitos adversos
Metformina/farmacocinética
Gravidez
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Blood Glucose); 0 (Hypoglycemic Agents); 0 (Insulin); 9100L32L2N (Metformin); SX6K58TVWC (Glyburide)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171013
[Lr] Data última revisão:
171013
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170830
[St] Status:MEDLINE
[do] DOI:10.1080/17425255.2017.1372423


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[PMID]:28847125
[Au] Autor:Khalili H; Derakhshan N; Ghaffarpasand F; Heydari ST
[Ad] Endereço:Neurosurgery Department, Shiraz University of Medical Sciences, Shiraz, Iran.
[Ti] Título:In Reply to the Letter to the Editor Regarding "Effects of Oral Glibenclamide on Brain Contusion Volume and Functional Outcome of Patients with Moderate and Severe Traumatic Brain Injuries: A Randomized Double-Blind Placebo-Controlled Clinical Trial".
[So] Source:World Neurosurg;105:1021, 2017 09.
[Is] ISSN:1878-8769
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Método Duplo-Cego
Glibureto
[Mh] Termos MeSH secundário: Contusão Encefálica
Lesões Encefálicas
Lesões Encefálicas Traumáticas
Contusões
Seres Humanos
Resultado do Tratamento
[Pt] Tipo de publicação:LETTER; COMMENT
[Nm] Nome de substância:
SX6K58TVWC (Glyburide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170914
[Lr] Data última revisão:
170914
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170830
[St] Status:MEDLINE



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