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[PMID]:29318321
[Au] Autor:Ziaie M; Dilmaghani KA; Tukmechi A
[Ti] Título:Synthesis and Biological Evaluation of 1,2,4-Triazoles and 1,3,4-Oxadiazoles Derivatives Linked to 1,4-Dihydropyridines Scaffold.
[So] Source:Acta Chim Slov;64(4):895-901, 2017 Dec.
[Is] ISSN:1318-0207
[Cp] País de publicação:Slovenia
[La] Idioma:eng
[Ab] Resumo:A series of diethyl-2,6-dimethyl-4-phenyl-1,4-dihydropyridine-3,5-dicarboxylate derivative coupled to 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones moieties at C2,C6 positions of 1,4-dihydropyridine ring system was prepared. This linkage was carried out by the reaction of 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones with 2,6-dibromomethyl-3,5-diethoxycarbonyl-4-phenyl-1,4-dihydropyridine in the presence of potassium carbonate as a weak base and dry acetone as the solvent. The newly synthesized compounds were characterized by FT-IR, 1H NMR, 13C NMR spectral data, elemental analysis and FAB-MS. The synthesized compounds were tested for their antimicrobial and antifungal activity against Escherichia coli and Aspergillus fumigatus in vitro in comparison with Enrofloxacin and Amphotericin as the reference drugs which are normally used for treating such infections. The synthetic compounds showed different inhibition zones against tested bacteria and fungi. Compound 8d showed more antagonistic activity against E. coli and A. fumigatus.
[Mh] Termos MeSH primário: Anti-Infecciosos/síntese química
Di-Hidropiridinas/química
Oxidiazóis/química
Triazóis/química
[Mh] Termos MeSH secundário: Anti-Infecciosos/farmacologia
Di-Hidropiridinas/farmacologia
Espectroscopia de Ressonância Magnética
Testes de Sensibilidade Microbiana
Oxidiazóis/farmacologia
Espectroscopia de Infravermelho com Transformada de Fourier
Triazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Dihydropyridines); 0 (Oxadiazoles); 0 (Triazoles)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180111
[St] Status:MEDLINE


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[PMID]:29324339
[Au] Autor:Azzouz R; Peauger L; Gembus V; Tîntas ML; Sopková-de Oliveira Santos J; Papamicaël C; Levacher V
[Ad] Endereço:VFP Therapies, 15 rue François Couperin, 76000 Rouen, France.
[Ti] Título:Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine "bio-oxidizable" prodrugs: Synthesis, biological evaluation and structure-activity relationship.
[So] Source:Eur J Med Chem;145:165-190, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:As an extension of our previous work on donepezil-based "bio-oxidizable" prodrug approach, two new classes of N-benzylpyridinium donepezil analogues in tetralone B2 and acetophenone B3 series and a new set of indanone derivatives B1 were investigated along with the corresponding dihydropyridine prodrugs A1-3. A total of fifty one N-benzylpyridinium quaternary donepezil analogues B1-3 and twenty two prodrugs A1-3 were synthesized and evaluated for their inhibitory activities against hAChE and eqBuChE. While most prodrugs A1-3 were demonstrated to be inactive against AChE (IC > 10 µM), a large number of the corresponding N-benzylpyridinium salt B1-3 exhibited appealing three-to-one-digit nanomolar hAChE inhibitory activities and even reaching subnanomolar activity (IC = 0.36 nM). In addition, in silico docking studies were conducted for several compounds to explain the more relevant in vitro results. Lastly, the influence of the two stereogenic centers in prodrugs A was also evaluated, highlighting not only marked differences in residual AChE inhibitory activity of the four separated isomers of prodrug 23h (IC ranging from 173 nM to 10 µM) but also significant variations of the oxidation rate between two separated diastereoisomers of prodrug 24a. This work provides useful information in the search of a preclinical candidate to conduct further development of this attractive "bio-oxidizable" prodrug strategy.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Inibidores da Colinesterase/farmacologia
Di-Hidropiridinas/farmacologia
Pró-Fármacos/farmacologia
Compostos de Piridínio/farmacologia
[Mh] Termos MeSH secundário: Animais
Butirilcolinesterase/metabolismo
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Di-Hidropiridinas/química
Relação Dose-Resposta a Droga
Electrophorus
Cavalos
Simulação de Acoplamento Molecular
Estrutura Molecular
Pró-Fármacos/síntese química
Pró-Fármacos/química
Compostos de Piridínio/síntese química
Compostos de Piridínio/química
Sais/síntese química
Sais/química
Sais/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Dihydropyridines); 0 (Prodrugs); 0 (Pyridinium Compounds); 0 (Salts); 7M8K3P6I89 (1,4-dihydropyridine); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180112
[St] Status:MEDLINE


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[PMID]:29269711
[Au] Autor:Kiuchi S; Hisatake S; Kabuki T; Oka T; Dobashi S; Fujii T; Ikeda T
[Ad] Endereço:Department of Cardiovascular Medicine, Toho University Faculty of Medicine.
[Ti] Título:Effect of Switching from Cilnidipine to Azelnidipine on Cardiac Sympathetic Nerve Function in Patients with Heart Failure Preserved Ejection Fraction.
[So] Source:Int Heart J;59(1):120-125, 2018 Jan 27.
[Is] ISSN:1349-3299
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Cardiac sympathetic nerve activity is known to play a key role in the development and progression of heart failure (HF). Azelnidipine, an L-type calcium channel blocker (CCB), inhibits the sympathetic nerve activity of the central system. In contrast, cilnidipine, an N-type CCB, inhibits the sympathetic nerve activity of the peripheral system. CCBs are recommended as class IIa in patients with HF preserved ejection fraction (HFpEF); however, there are no comparative data on the difference in effect of cilnidipine and azelnidipine in patients with HFpEF and hypertension. We investigated the difference in effect of azelnidipine compared with cilnidipine in patients with HFpEF. Twenty-four consecutive HF patients who received angiotensin II type1a receptor blocker and beta blocker from April 2013 to January 2015 were enrolled. Cilnidipine was switched to azelnidipine during the follow-up period. Blood pressures, heart rate, blood tests, echocardiography, and I-metaiodobenzylguanidine (MIBG) cardiac-scintigraphy were measured before and after 6 months from azelnidipine administration. B-type natriuretic peptide tended to decrease after switching to azelnidipine; however, there were no significant differences between the pre-state and post-state (pre-state: 118.5 pg/mL and post-state: 78.4 pg/mL, P = 0.137). Other laboratory findings, including catecholamine, also did not change significantly. In echocardiography, there were no significant differences in systolic and diastolic functions at the pre-state and post-state. As for MIBG, there were no significant changes in heart/mediastinum ratio. However, washout rate was significantly reduced (pre-state: 42.9 and post-state: 39.6, P = 0.030). Azelnidipine improved the dysfunction of cardiac sympathetic nerve activity compared with cilnidipine in patients with HFpEF.
[Mh] Termos MeSH primário: Ácido Azetidinocarboxílico/análogos & derivados
Di-Hidropiridinas/administração & dosagem
Substituição de Medicamentos
Insuficiência Cardíaca/tratamento farmacológico
Coração/inervação
Volume Sistólico/efeitos dos fármacos
Sistema Nervoso Simpático/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Ácido Azetidinocarboxílico/administração & dosagem
Bloqueadores dos Canais de Cálcio/administração & dosagem
Relação Dose-Resposta a Droga
Ecocardiografia
Feminino
Seguimentos
Insuficiência Cardíaca/diagnóstico
Insuficiência Cardíaca/fisiopatologia
Seres Humanos
Masculino
Meia-Idade
Cintilografia/métodos
Estudos Retrospectivos
Sistema Nervoso Simpático/fisiopatologia
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Dihydropyridines); 2517-04-6 (Azetidinecarboxylic Acid); 97T5AZ1JIP (cilnidipine); PV23P19YUG (azelnidipine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180206
[Lr] Data última revisão:
180206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171223
[St] Status:MEDLINE
[do] DOI:10.1536/ihj.17-024


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[PMID]:29199222
[Au] Autor:Hosaka S; Tokunaga Y
[Ad] Endereço:Research and Development Division, Sawai Pharmaceutical Co., Ltd.
[Ti] Título:Differences in Powder Properties of Two 1,4-Dihydropyridine-Type Compounds Evaluated through Thermal Analysis.
[So] Source:Chem Pharm Bull (Tokyo);65(12):1175-1178, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The powder properties of two 1,4-dihydropyridine type compounds, manidipine dihydrochloride (Man) and benidipine hydrochloride (Ben), which possess similar physicochemical properties, were compared through thermal and mechanical analyses. Man and Ben were compressed with lactose monohydrate (Lac) and magnesium stearate (Mgst) at different compression forces. As an index, we focused on the onset temperatures of Lac dehydration during thermal analysis and plotted them against compression forces to evaluate the differences in powder properties between Man and Ben. To discuss in detail, the Lac ratio was selected as a formulation factor and compression speed as a process factor, which would be influenced to the onset temperature or its profile. It could be represented that Man was more adherent than Ben through thermal analysis by changing these critical factors, which were consistent with the results obtained through mechanical analysis.
[Mh] Termos MeSH primário: Di-Hidropiridinas/química
Nifedipino/análogos & derivados
[Mh] Termos MeSH secundário: Varredura Diferencial de Calorimetria
Força Compressiva
Lactose/química
Nifedipino/química
Ácidos Esteáricos/química
Comprimidos/química
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dihydropyridines); 0 (Stearic Acids); 0 (Tablets); 0A6746FWDL (benidipine hydrochloride); 4ELV7Z65AP (stearic acid); 6O4754US88 (manidipine); I9ZF7L6G2L (Nifedipine); J2B2A4N98G (Lactose)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180110
[Lr] Data última revisão:
180110
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171205
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00375


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[PMID]:28966273
[Au] Autor:El-Moselhy TF; Sidhom PA; Esmat EA; El-Mahdy NA
[Ad] Endereço:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Tanta University.
[Ti] Título:Synthesis, Docking Simulation, Biological Evaluations and 3D-QSAR Study of 1,4-Dihydropyridines as Calcium Channel Blockers.
[So] Source:Chem Pharm Bull (Tokyo);65(10):893-903, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Resurgence to target L-type voltage-dependent calcium channels has been applied by the synthesis of two series of nifedipine analogues where the ortho- or a meta-nitrophenyl ring is retained. A pre-synthetic molecular docking study with a receptor model followed by molecular alignment has been performed on 47 compounds to predict the most active member. The IC values revealed that some of the compounds are similar to or more active than nifedipine. Substitution of groups at the 3- and 5-positions of the dihydropyridine (DHP) ring gave 3k, which is more active than nifedipine. Our valid three-dimensional quantitative structure-activity relationship (3D-QSAR) model prefigures the influence of lipophilicity, bulkiness and chelating effects of the C3 and C5 substituents. Bulky groups interfere with ring-to-ring hydrophobic interaction with tyrosine (Tyr) and limit the efficiency of increasing the length of the hydrocarbon chain of esters at the 3- and 5-positions of the DHP ring as an approach to increasing the activity. The presence of a chelating substituent on the phenyl ring at the 4-position of the DHP ring ensures strong binding to the receptor and hence stabilization of the closed-channel conformation. The validation of 3D-QSAR model indicated its proficiency in predicting activity of newly compounds belonging to the same chemical class.
[Mh] Termos MeSH primário: Bloqueadores dos Canais de Cálcio/síntese química
Di-Hidropiridinas/química
Di-Hidropiridinas/síntese química
[Mh] Termos MeSH secundário: Animais
Arcobacter/metabolismo
Proteínas de Bactérias/metabolismo
Sítios de Ligação
Bloqueadores dos Canais de Cálcio/química
Bloqueadores dos Canais de Cálcio/metabolismo
Canais de Cálcio Tipo L/química
Canais de Cálcio Tipo L/metabolismo
Di-Hidropiridinas/metabolismo
Concentração Inibidora 50
Simulação de Acoplamento Molecular
Estrutura Terciária de Proteína
Relação Quantitativa Estrutura-Atividade
Coelhos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Calcium Channel Blockers); 0 (Calcium Channels, L-Type); 0 (Dihydropyridines); 0 (L-type calcium channel alpha(1C)); 7M8K3P6I89 (1,4-dihydropyridine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171003
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00186


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[PMID]:28858832
[Au] Autor:Gündüz MG; Ragno G; Simsek R; De Luca M; Safak C; Grande F; El-Khouly A; Isli F; Yildirim S; Öztürk Fincan GS; Ioele G
[Ad] Endereço:.
[Ti] Título:Synthesis and photodegradation studies of analogues of muscle relaxant 1,4-dihydropyridine compounds.
[So] Source:Acta Pharm;67(3):341-355, 2017 Sep 01.
[Is] ISSN:1846-9558
[Cp] País de publicação:Croatia
[La] Idioma:eng
[Ab] Resumo:This paper describes the synthesis of 1,4-dihydropyridine compounds (DHPs) endowed with good muscle relaxant activity and stability to light. Six new condensed DHPs were synthesized by the microwave irradiation method. A long-chain ester moiety [2-(methacryloyloxy)ethyl] and various substituents on the phenyl ring were demonstrated to affect the muscle relaxant activity occurring in isolated rabbit gastric fundus smooth muscle strips. Forced photodegradation conditions were applied to the molecules according to the ICH rules. The degradation profile of the drugs was monitored by spectrophotometry coupled with the multivariate curve resolution technique. Formation of the oxidized pyridine derivative was observed for all the studied DHPs, except for one compound, which showed very fast degradation and formation of a second photo-product. Pharmacological tests on the molecules showed a good muscle relaxing effect, with a mechanism similar to that of nifedipine, however, proving to be more stable to light.
[Mh] Termos MeSH primário: Di-Hidropiridinas/química
Músculo Liso/efeitos dos fármacos
Fármacos Neuromusculares/química
[Mh] Termos MeSH secundário: Animais
Técnicas In Vitro
Luz
Fotólise
Coelhos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dihydropyridines); 0 (Neuromuscular Agents); 7M8K3P6I89 (1,4-dihydropyridine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE


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[PMID]:28836855
[Au] Autor:Chamsai B; Limmatvapirat S; Sungthongjeen S; Sriamornsak P
[Ad] Endereço:a Department of Pharmaceutical Technology, Faculty of Pharmacy , Silpakorn University , Nakhon Pathom , Thailand.
[Ti] Título:Enhancement of solubility and oral bioavailability of manidipine by formation of ternary solid dispersion with d-α-tocopherol polyethylene glycol 1000 succinate and copovidone.
[So] Source:Drug Dev Ind Pharm;43(12):2064-2075, 2017 Dec.
[Is] ISSN:1520-5762
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Low bioavailability of oral manidipine (MDP) is due to its low water solubility. OBJECTIVE: The objective of this study was to increase the solubility and bioavailability of MDP by fabricating ternary solid dispersion (tSD) with d-α-tocopherol polyethyleneglycol-1000-succinate and copovidone. METHODS: In this study, solid ternary phase diagram was applied in order to check the homogeneity of tSD prepared by melting and solidifying with dry ice. The physicochemical properties of different formulations were determined by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and hot stage microscopy. Their solubility, dissolution, stability and bioavailability were also investigated. RESULTS AND DISCUSSION: The results demonstrated that tSD obtained from ternary phase diagram divided into homogeneous and non-homogeneous regions. In the homogenous region, the transparent characteristics of tSD was observed and considered as a glass solution, which have a higher MDP solubility than that in non-homogenous region. The hot stage microscopy, DSC and PXRD confirmed that solid dispersion was formed in which MDP was molecularly dispersed in the carriers, especially in the homogenous region of phase diagram. FTIR analysis demonstrated strong hydrogen bonding between amine groups of MDP and carbonyl groups of copovidone, which supported a higher solubility and dissolution of tSD. The pharmacokinetic study in Wistar rats showed that the tSD had the greatest effect on oral bioavailability. Immediate hypotensive effect of tSD was also observed in vivo. CONCLUSIONS: The improvement of stability, dissolution and oral bioavailability of MDP could be achieved by using tSD technique.
[Mh] Termos MeSH primário: Di-Hidropiridinas/química
Di-Hidropiridinas/farmacocinética
Polietilenoglicóis/química
Pirrolidinas/química
Succinatos/química
Compostos de Vinila/química
alfa-Tocoferol/química
alfa-Tocoferol/farmacocinética
[Mh] Termos MeSH secundário: Animais
Disponibilidade Biológica
Varredura Diferencial de Calorimetria
Pós
Ratos
Ratos Wistar
Solubilidade
Espectroscopia de Infravermelho com Transformada de Fourier
Difração de Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dihydropyridines); 0 (Powders); 0 (Pyrrolidines); 0 (Succinates); 0 (Vinyl Compounds); 0 (poly(vinylpyrrolidone-co-vinyl-acetate)); 30IQX730WE (Polyethylene Glycols); 6O4754US88 (manidipine); H4N855PNZ1 (alpha-Tocopherol); U076Q6Q621 (polyethylene glycol 1000)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171018
[Lr] Data última revisão:
171018
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170825
[St] Status:MEDLINE
[do] DOI:10.1080/03639045.2017.1371731


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[PMID]:28640864
[Au] Autor:Naziroglu M; Çig B; Blum W; Vizler C; Buhala A; Marton A; Katona R; Jósvay K; Schwaller B; Oláh Z; Pecze L
[Ad] Endereço:Neuroscience Research Center, Suleyman Demirel University, Isparta, Turkey.
[Ti] Título:Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels.
[So] Source:PLoS One;12(6):e0179950, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity. However, capsaicin cannot be given systemically in large doses, because of its induction of acute pain and neurological inflammation. MRS1477, a dihydropyridine derivative acts as a positive allosteric modulator of TRPV1, if added together with capsaicin, but is ineffective, if given alone. Addition of MRS1477 evoked Ca2+ signals in MCF7 breast cancer cells, but not in primary breast epithelial cells. This indicates that MCF7 cells not only express functional TRPV1 channels, but also produce endogenous TRPV1 agonists. We investigated the effects of MRS1477 and capsaicin on cell viability, caspase-3 and -9 activities and reactive oxygen species production in MCF7 cells. The fraction of apoptotic cells was increased after 3 days incubation with capsaicin (10 µM) paralleled by increased reactive oxygen species production and caspase activity. These effects were even more pronounced, when cells were incubated with MRS1477 (2 µM) either alone or together with CAPS (10 µM). Capsazepine, a TRPV1 blocker, inhibited both the effect of capsaicin and MRS1477. Whole-cell patch clamp recordings revealed that capsaicin-evoked TRPV1-mediated current density levels were increased after 3 days incubation with MRS1477 (2 µM). However, the tumor growth in MCF7 tumor-bearing immunodeficient mice was not significantly decreased after treatment with MRS1477 (10 mg/ kg body weight, i.p., injection twice a week). In conclusion, in view of a putative in vivo treatment with MRS1477 or similar compounds further optimization is required.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Neoplasias da Mama/patologia
Di-Hidropiridinas/farmacologia
Terapia de Alvo Molecular
Canais de Cátion TRPV/metabolismo
[Mh] Termos MeSH secundário: Regulação Alostérica/efeitos dos fármacos
Animais
Apoptose/efeitos dos fármacos
Sinalização do Cálcio/efeitos dos fármacos
Capsaicina/farmacologia
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Interações Medicamentosas
Seres Humanos
Células MCF-7
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Camundongos
Estresse Oxidativo/efeitos dos fármacos
Espécies Reativas de Oxigênio/metabolismo
Microambiente Tumoral/efeitos dos fármacos
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4,5-diethyl-3-(2-methoxyethylthio)-2-methyl-6-phenyl-1,4-dihydropyridine-3,5-dicarboxylate); 0 (Antineoplastic Agents); 0 (Dihydropyridines); 0 (Reactive Oxygen Species); 0 (TRPV Cation Channels); 0 (TRPV1 protein, human); S07O44R1ZM (Capsaicin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170918
[Lr] Data última revisão:
170918
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170623
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0179950


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[PMID]:28636634
[Au] Autor:Mitrega KA; Spalek AM; Nozynski J; Porc M; Stankiewicz M; Krzeminski TF
[Ad] Endereço:Silesian Centre for Heart Diseases, Zabrze, Poland.
[Ti] Título:Cardiomyopathy development protection after myocardial infarction in rats: Successful competition for major dihydropyridines' common metabolite against captopril.
[So] Source:PLoS One;12(6):e0179633, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:During the last 25 years angiotensin-converting enzyme inhibitors spectacularly conquered the field of cardiovascular diseases therapy. Nevertheless, lack of new studies concerning side effects associated with their chronic administration seems to be rather confusing. In our previous research, we proved that the main furnidipines' metabolite (M-2) possess multiple cardioprotective actions. Currently, we compared effects of post-infarction long-term oral treatment with M-2 and captopril on hemodynamic parameters and "ischemic cardiomyopathy" development in rats. Myocardial infarction was evoked by permanent left anterior descending coronary artery occlusion for 35 days. Surviving rats were treated with captopril (2 × 25 mg/kg) or M-2 (4 mg/kg) from 6th- 35th day. At 35th day rats' hearts were tested on working heart setup, where following parameters were measured: heart rate, preload pressure, aortic systolic and diastolic pressures, aortic maximum rise and fall, aortic and coronary flow, myocardial oxygen consumption and oximetry in perfusate. Subsequently, heart tissue specimens were assessed during morphological estimation. Captopril caused significant heart rate increase and markedly diminished preload pressure in comparison to M-2. Both drugs evoked essential aortic pressure increase. Aortic flow was significantly decreased after M-2, whereas captopril increased this parameter in comparison to M-2. Both agents caused marked coronary flow increase. Morphologic examination in captopril revealed cardiomyopathic process in 70% of hearts, whereas in M-2 this value reached 30%. Neovascularization of post-infarcted myocardium was visible only after M-2 therapy. Concluding, M-2 presented itself as more attractive agent in long-term post-infarction treatment by preventing cardiomyopathy development, angiogenesis stimulation and preserving cardiac performance.
[Mh] Termos MeSH primário: Inibidores da Enzima Conversora de Angiotensina/uso terapêutico
Captopril/uso terapêutico
Cardiomiopatias/prevenção & controle
Di-Hidropiridinas/metabolismo
Infarto do Miocárdio/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Oral
Inibidores da Enzima Conversora de Angiotensina/farmacologia
Animais
Biomarcadores/sangue
Pressão Sanguínea/efeitos dos fármacos
Captopril/farmacologia
Cardiomiopatias/etiologia
Di-Hidropiridinas/farmacologia
Di-Hidropiridinas/uso terapêutico
Modelos Animais de Doenças
Coração/fisiopatologia
Frequência Cardíaca/efeitos dos fármacos
Hemodinâmica/efeitos dos fármacos
Masculino
Infarto do Miocárdio/mortalidade
Infarto do Miocárdio/patologia
Miocárdio/patologia
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Angiotensin-Converting Enzyme Inhibitors); 0 (Biomarkers); 0 (Dihydropyridines); 9G64RSX1XD (Captopril)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170622
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0179633


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[PMID]:28554730
[Au] Autor:Wang M; Gao M; Meyer JA; Peters JS; Zarrinmayeh H; Territo PR; Hutchins GD; Zheng QH
[Ad] Endereço:Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202, USA.
[Ti] Título:Synthesis and preliminary biological evaluation of radiolabeled 5-BDBD analogs as new candidate PET radioligands for P2X4 receptor.
[So] Source:Bioorg Med Chem;25(14):3835-3844, 2017 Jul 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:P2X4 receptor has become an interesting molecular target for treatment and PET imaging of neuroinflammation and associated brain diseases such as Alzheimer's disease. This study reports the first design, synthesis, radiolabeling and biological evaluation of new candidate PET P2X4 receptor radioligands using 5-BDBD, a specific P2X4 receptor antagonist, as a scaffold. 5-(3-Hydroxyphenyl)-1-[ C]methyl-1,3-dihydro-2H-benzofuro[3,2-e][1,4]diazepin-2-one (N-[ C]Me-5-BDBD analog, [ C]9) and 5-(3-Bromophenyl)-1-[ C]methyl-1,3-dihydro-2H-benzofuro[3,2-e][1,4]diazepin-2-one (N-[ C]Me-5-BDBD, [ C]8c) were prepared from their corresponding desmethylated precursors with [ C]CH OTf through N-[ C]methylation and isolated by HPLC combined with SPE in 30-50% decay corrected radiochemical yields with 370-1110GBq/µmol specific activity at EOB. 5-(3-[ F]Fluorophenyl)-1,3-dihydro-2H-benzofuro[3,2-e][1,4]diazepin-2-one ([ F]F-5-BDBD, [ F]5a) and 5-(3-(2-[ F]fluoroethoxy)phenyl)-1,3-dihydro-2H-benzofuro[3,2-e][1,4]diazepin-2-one ([ F]FE-5-BDBD, [ F]11) were prepared from their corresponding nitro- and tosylated precursors by nucleophilic substitution with K[ F]F/Kryptofix 2.2.2 and isolated by HPLC-SPE in 5-25% decay corrected radiochemical yields with 111-740GBq/µmol specific activity at EOB. The preliminary biological evaluation of radiolabeled 5-BDBD analogs indicated these new radioligands have similar biological activity with their parent compound 5-BDBD.
[Mh] Termos MeSH primário: Azirinas/química
Di-Hidropiridinas/química
Compostos Radiofarmacêuticos/síntese química
Receptores Purinérgicos P2X4/metabolismo
[Mh] Termos MeSH secundário: Trifosfato de Adenosina/química
Trifosfato de Adenosina/metabolismo
Azirinas/síntese química
Azirinas/metabolismo
Ligação Competitiva
Radioisótopos de Carbono/química
Di-Hidropiridinas/síntese química
Di-Hidropiridinas/metabolismo
Radioisótopos de Flúor/química
Células HEK293
Seres Humanos
Marcação por Isótopo
Tomografia por Emissão de Pósitrons
Ligação Proteica
Compostos Radiofarmacêuticos/química
Compostos Radiofarmacêuticos/metabolismo
Receptores Purinérgicos P2X4/química
Receptores Purinérgicos P2X4/genética
Proteínas Recombinantes/biossíntese
Proteínas Recombinantes/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azirines); 0 (Carbon Radioisotopes); 0 (Dihydropyridines); 0 (Fluorine Radioisotopes); 0 (Radiopharmaceuticals); 0 (Receptors, Purinergic P2X4); 0 (Recombinant Proteins); 135330-18-6 (diazipine); 8L70Q75FXE (Adenosine Triphosphate)
[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:170531
[St] Status:MEDLINE



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