Base de dados : MEDLINE
Pesquisa : D02.455.326.146.485 [Categoria DeCS]
Referências encontradas : 541 [refinar]
Mostrando: 1 .. 10   no formato [Detalhado]

página 1 de 55 ir para página                         

  1 / 541 MEDLINE  
              next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28574799
[Au] Autor:Kumamoto H; Fukano M; Imoto S; Kohgo S; Odanaka Y; Amano M; Kuwata-Higashi N; Mitsuya H; Haraguchi K; Fukuhara K
[Ad] Endereço:a School of Pharmacy , Showa University , Shinagawa-ku , Tokyo , Japan.
[Ti] Título:A novel entecavir analogue constructing with a spiro[2.4]heptane core structure in the aglycon moiety: Its synthesis and evaluation for anti-hepatitis B virus activity.
[So] Source:Nucleosides Nucleotides Nucleic Acids;36(7):463-473, 2017 Jul 03.
[Is] ISSN:1532-2335
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Synthesis of a novel 2'-deoxy-guanine carbocyclic nucleoside 4 constructed with spiro[2.4]heptane core structure in the aglycon moiety was carried out. Radical-mediated 5-exo-dig mode cyclization and following cyclopropanation proceeded efficiently to furnish the spiro alcohol 10. Subsequent Mitsunobu-type glycosylation between 13 and 14, deoxygenation of the 2'-hydroxyl group of 16 and deprotection of 17 gave the title compound 4. Compound 4 demonstrated moderate anti-HBV activity (EC value of 0.12 ± 0.02 µM) and no cytotoxicity against HepG2 cells was observed up to 100 µM.
[Mh] Termos MeSH primário: Antivirais/química
Antivirais/farmacologia
Guanina/análogos & derivados
Vírus da Hepatite B/efeitos dos fármacos
Heptanos/química
[Mh] Termos MeSH secundário: Antivirais/síntese química
Técnicas de Química Sintética
Guanina/síntese química
Guanina/química
Guanina/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Heptanes); 5968Y6H45M (entecavir); 5Z93L87A1R (Guanine)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170603
[St] Status:MEDLINE
[do] DOI:10.1080/15257770.2017.1322209


  2 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28426179
[Au] Autor:Micheli F
[Ad] Endereço:Aptuit Verona s.r.l., Medicines Research Centre, Via Fleming 4, 37135, Verona, Italy.
[Ti] Título:Novel, Selective, and Developable Dopamine D Antagonists with a Modified "Amino" Region.
[So] Source:ChemMedChem;12(16):1254-1260, 2017 Aug 22.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:This Minireview describes a presentation made at the XXIV National Meeting in Medicinal Chemistry (NMMC) held in Perugia (Italy), September 11-14, 2016. It relates to the discovery of novel templates of the so-called "amino" region of dopamine D receptor antagonists. Moving from the early scaffolds, which were modified in the amine portion, this review discusses the variations that led to the discovery of new systems published in 2016, which allowed the identification of compounds endowed with great selectivity over the dopamine D receptor and the human ether-à-go-go-related gene (hERG) ion channel. The main efforts in characterizing these compounds were devoted not only to determining their potency and selectivity relative to closely associated targets (e.g., the dopamine D receptor), but to ensure a large therapeutic window versus liability points such as hERG. In particular, we present examples of derivatives with selectivities greater than 2000-fold. Furthermore, much focus is devoted to the overall developability of the scaffolds, ensuring that appropriate physicochemical and pharmacokinetic parameters are present in all compounds progressing through the screening cascade.
[Mh] Termos MeSH primário: Antagonistas de Dopamina/química
Receptores de Dopamina D3/metabolismo
[Mh] Termos MeSH secundário: Antagonistas de Dopamina/metabolismo
Desenho de Drogas
Heptanos/química
Heptanos/metabolismo
Seres Humanos
Morfolinas/química
Morfolinas/metabolismo
Ligação Proteica
Pirróis/química
Pirróis/metabolismo
Receptores de Dopamina D2/química
Receptores de Dopamina D2/metabolismo
Receptores de Dopamina D3/antagonistas & inibidores
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Dopamine Antagonists); 0 (Heptanes); 0 (Morpholines); 0 (Pyrroles); 0 (Receptors, Dopamine D2); 0 (Receptors, Dopamine D3); 8B2ZCK305O (morpholine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170421
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700148


  3 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28179081
[Au] Autor:Müller M; Englert M; Earle MJ; Vetter W
[Ad] Endereço:University of Hohenheim, Institute of Food Chemistry, Department of Food Chemistry (170b), D-70593 Stuttgart, Germany.
[Ti] Título:Development of solvent systems with room temperature ionic liquids for the countercurrent chromatographic separation of very nonpolar lipid compounds.
[So] Source:J Chromatogr A;1488:68-76, 2017 Mar 10.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Solvent systems are not readily available for the separation of very nonpolar compounds by countercurrent chromatography (CCC). In this study we therefore evaluated the suitability of room temperature ionic liquids (IL) in organic solvents for the CCC separation of the extremely nonpolar lipid compounds tripalmitin (PPP) and cholesteryl stearate (CS). The four IL tested were [C mim][OTf], [C mim][NTf ], [P66614][NTf ], and [P66614][Cl]. Search for a CCC-suited solvent system started with solubility studies with fourteen organic solvents. Following this, combinations were made with one organic solvent miscible and one organic solvent immiscible with IL (147 combinations). Twenty-four initially monophasic mixtures of two organic solvents became biphasic by adding IL. Several unexpected results could be observed. For instance, n-hexane and n-heptane became biphasic with [P66614][Cl]. Further nine systems became biphasic although the IL was not miscible in any of the two components. These 33 solvent systems were investigated with regard to phase ratio, settling time, share of IL in the upper phase and last not least the K values of PPP and CS, which were 8.1 and 7.7 respectively. The most promising system, n-heptane/chloroform/[C mim][OTf] (3:3:1, v/v/v) allowed a partial separation of PPP and CS by CCC which was not achieved beforehand.
[Mh] Termos MeSH primário: Distribuição Contracorrente/métodos
Líquidos Iônicos/química
Lipídeos/isolamento & purificação
Solventes/química
Temperatura Ambiente
[Mh] Termos MeSH secundário: Clorofórmio/química
Heptanos/química
Triglicerídeos/isolamento & purificação
Raios Ultravioleta
Viscosidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Heptanes); 0 (Ionic Liquids); 0 (Lipids); 0 (Solvents); 0 (Triglycerides); 456148SDMJ (n-heptane); 7V31YC746X (Chloroform); D133ZRF50U (tripalmitin)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170210
[St] Status:MEDLINE


  4 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28161126
[Au] Autor:Brace EC; Engelberth AS
[Ad] Endereço:Department of Agricultural & Biological Engineering, Purdue University, 125 S. State St., West Lafayette, IN 47907, United States; Laboratory of Renewable Resources Engineering, Purdue University, 500 Central Dr., West Lafayette, IN 47907, United States. Electronic address: ebrace@purdue.edu.
[Ti] Título:Enhancing silymarin fractionation using the conductor-like screening model for real solvents.
[So] Source:J Chromatogr A;1487:187-193, 2017 Mar 03.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A significant hurdle for discovery of plant-derived products is the numerous trial-and-error experiments required to develop an effective purification strategy. To overcome the experimental burden, a quantum mechanics-based molecular modeling approach - known as the COnductor-like Screening Model for Real Solvents (COSMO-RS) - was used to predict a suitable two-phase solvent system to purify six silymarins from an aqueous mixture. Silymarins, a class of flavonolignans found in milk thistle (Silybum marianum L.), are well suited for assessing the use of a molecular modeling approach to predict partitioning in a countercurrent chromatography (CCC) separation because they are well characterized and previous studies report low purity fractionation in liquid-liquid solvent systems. They also present an opportunity to evaluate the use of COSMO-RS in predicting the partitioning of structurally similar isomeric compounds that are present together in an aqueous solution upon extraction from their native source. The COSMO-RS model results predicted the partition coefficients in: three traditional ARIZONA solvent systems (composed of heptane, ethyl acetate, methanol, and water), nine additional variations of this quaternary solvent system, and two chloroform, methanol, and water solvent systems. Predicted results were concise but not accurate when compared to experimental results determined by the shake flask method. The 1:4:3:5 n-heptane:ethyl acetate:methanol:water (v/v/v/v) system was identified to be an improvement on the 1:4:3:4 system previously reported. The present study verified the ability of COSMO-RS to hone in on one or two solvent systems that will yield the best fractionation using CCC.
[Mh] Termos MeSH primário: Distribuição Contracorrente/métodos
Silimarina/isolamento & purificação
Solventes
[Mh] Termos MeSH secundário: Acetatos
Clorofórmio
Heptanos
Metanol
Cardo Mariano/química
Modelos Moleculares
Água
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetates); 0 (Heptanes); 0 (Silymarin); 0 (Solvents); 059QF0KO0R (Water); 456148SDMJ (n-heptane); 76845O8NMZ (ethyl acetate); 7V31YC746X (Chloroform); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170314
[Lr] Data última revisão:
170314
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170206
[St] Status:MEDLINE


  5 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:27780957
[Au] Autor:Takó M; KotogÁn A; Papp T; Kadaikunnan S; Alharbi NS; VÁgvölgyi C
[Ad] Endereço:Department of Microbiology, Faculty of Science and Informatics, University of Szeged, H-6726 Szeged, Közép fasor 52, Hungary.
[Ti] Título:Purification and Properties of Extracellular Lipases with Transesterification Activity and 1,3-Regioselectivity from and .
[So] Source:J Microbiol Biotechnol;27(2):277-288, 2017 Feb 28.
[Is] ISSN:1738-8872
[Cp] País de publicação:Korea (South)
[La] Idioma:eng
[Ab] Resumo:NRRL 5282 and NRRL 1526 can produce lipases with high synthetic activities in wheat bran-based solid-state culture. In this study, the purification and biochemical characterization of the lipolytic activities of these lipases are presented. SDS-PAGE indicated a molecular mass of about 55 and 35 kDa for the purified and enzymes, respectively. -Nitrophenyl palmitate ( NPP) hydrolysis was maximal at 40°C and pH 7.0 for the lipase, and at 30°C and pH 5.2 for the enzyme. The enzymes showed almost equal affinity to NPP, but the of the lipase was about 1.13 times higher than that determined for using the same substrate. For both enzymes, a dramatic loss of activity was observed in the presence of 5 mM Hg , Zn , or Mn , 10 mM -bromosuccinimide or sodium dodecyl sulfate, and 5-10% (v/v) of hexanol or butanol. At the same time, they proved to be extraordinarily stable in the presence of -hexane, cyclohexane, -heptane, and isooctane. Moreover, isopentanol up to 10% (v/v) and propionic acid in 1 mM concentrations increased the NPP hydrolyzing activity of lipase. Both enzymes had 1,3-regioselectivity, and efficiently hydrolyzed -nitrophenyl ( NP) esters with C8-C16 acids, exhibiting maximum activity towards NP-caprylate ( ) and pNP-dodecanoate ( ). The purified lipases are promising candidates for various biotechnological applications.
[Mh] Termos MeSH primário: Lipase/isolamento & purificação
Lipase/metabolismo
Rhizomucor/enzimologia
Rhizopus/enzimologia
[Mh] Termos MeSH secundário: Bromosuccinimida/farmacologia
Butanóis/farmacologia
Caprilatos/farmacologia
Eletroforese em Gel de Poliacrilamida
Esterificação
Heptanos/farmacologia
Hexanos/farmacologia
Hexanóis/farmacologia
Concentração de Íons de Hidrogênio
Hidrólise
Cinética
Lauratos/farmacologia
Lipase/química
Manganês/farmacologia
Mercúrio/farmacologia
Nitrobenzenos/farmacologia
Palmitatos/metabolismo
Propionatos/farmacologia
Rhizomucor/genética
Rhizopus/genética
Dodecilsulfato de Sódio/farmacologia
Zinco/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-nitrophenyl dodecanoate); 0 (Butanols); 0 (Caprylates); 0 (Heptanes); 0 (Hexanes); 0 (Hexanols); 0 (Laurates); 0 (Nitrobenzenes); 0 (Palmitates); 0 (Propionates); 1492-30-4 (4-nitrophenyl palmitate); 1956-10-1 (4-nitrophenyloctanoate); 2DDG612ED8 (n-hexane); 368GB5141J (Sodium Dodecyl Sulfate); 42Z2K6ZL8P (Manganese); 456148SDMJ (n-heptane); EC 3.1.1.3 (Lipase); FXS1BY2PGL (Mercury); J41CSQ7QDS (Zinc); JHU490RVYR (propionic acid); K8G1F2UCJF (Bromosuccinimide)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170328
[Lr] Data última revisão:
170328
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161027
[St] Status:MEDLINE
[do] DOI:10.4014/jmb.1608.08005


  6 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:27629801
[Au] Autor:Crosley DR; Araps CJ; Doyle-Eisele M; McDonald JD
[Ad] Endereço:a Private consultant to HGI Industries (Boynton Beach, Florida) , Palo Alto , CA , USA.
[Ti] Título:Gas-phase photolytic production of hydroxyl radicals in an ultraviolet purifier for air and surfaces.
[So] Source:J Air Waste Manag Assoc;67(2):231-240, 2017 Feb.
[Is] ISSN:2162-2906
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We have measured the concentration of hydroxyl radicals (OH) produced in the gas phase by a commercially available purifier for air and surfaces, using the time rate of decay of n-heptane added to an environmental chamber. The hydroxyl generator, an Odorox® BOSS™ model, produces the OH through 185-nm photolysis of ambient water vapor. The steady-state concentration of OH produced in the 120 m chamber is, with 2σ error bars, (3.25 ± 0.80) × 10 cm . The properties of the hydroxyl generator, in particular the output of the ultraviolet lamps and the air throughput, together with an estimation of the water concentration, were used to predict the amount of OH produced by the device, with no fitted parameters. To relate this calculation to a steady-state concentration, we must estimate the OH loss rate within the chamber owing to reaction with the n-heptane and the 7 ppb of background hydrocarbons that are present. The result is a predicted steady-state concentration in excellent agreement with the measured value. This shows we understand well the processes occurring in the gas phase during operation of this hydroxyl radical purifier. IMPLICATIONS: Hydroxyl radical air purifiers are used for cleaning both gaseous contaminants, such as volatile organic compounds (VOCs) or hazardous gases, and biological pathogens, both airborne and on surfaces. This is the first chemical kinetic study of such a purifier that creates gas-phase OH by ultraviolet light photolysis of H O. It shows that the amount of hydroxyls produced agrees well with nonparameterized calculations using the purifier lamp output and device airflow. These results can be used for designing appropriate remediation strategies.
[Mh] Termos MeSH primário: Radical Hidroxila/química
Raios Ultravioleta
[Mh] Termos MeSH secundário: Heptanos/química
Cinética
Ozônio/química
Fotólise
Compostos Orgânicos Voláteis
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Heptanes); 0 (Volatile Organic Compounds); 3352-57-6 (Hydroxyl Radical); 456148SDMJ (n-heptane); 66H7ZZK23N (Ozone)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170804
[Lr] Data última revisão:
170804
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160916
[St] Status:MEDLINE
[do] DOI:10.1080/10962247.2016.1229236


  7 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:28314431
[Au] Autor:Russo MV; Avino P; Notardonato I
[Ad] Endereço:Department of Agriculture, Environment and Food, University of Molise, via De Sanctis, I-86100 Campobasso, Italy. Electronic address: mvrusso@unimol.it.
[Ti] Título:Fast analysis of phthalates in freeze-dried baby foods by ultrasound-vortex-assisted liquid-liquid microextraction coupled with gas chromatography-ion trap/mass spectrometry.
[So] Source:J Chromatogr A;1474:1-7, 2016 Nov 25.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This paper is focused on the determination of phthalates (PAEs), compounds "plausibly" endocrine disruptors, in baby food products by means of a method based on ultrasound-vortex-assisted liquid-liquid microextraction coupled with GC-IT/MS (UVALLME-GC-IT/MS). Particularly, the whole procedure allows the determination of six phthalates such as DMP, DEP, DBP, iBcEP, BBP and DEHP. After dissolution of 0.1g product sample and addition of anthracene as Internal Standard, 250µL of n-heptane are used as extraction solvent. The solution, held for 5min on the vortex mixer and for 6min in an ultrasonic bath at 100W for favoring the solvent dispersion and consequently the analyte extraction, is centrifuged at 4000rpm for 30min. About 100µL of heptane are recovered and 1µL is injected into the GC-IT/MS. All the analytical parameters investigated are deeply discussed: under the best conditions, the percentage recoveries range between 96.2 and 109.2% with an RSD ≤10.5% whereas the Limit of Detections (LODs) and the Limit of Quantifications (LOQs) are below 11 and 20ngg , respectively, for all the PAEs except for iBcEP (23 and 43ngg , respectively). The linear dynamic range of this procedure is between 10 and 5000ngg with R ≥0.92. The method has been applied to real commercial freeze-dried samples (chicken and turkey meats) available on the Italian pharmaceutical market: three PAEs were preliminary identified, i.e. DEP (14ngg ), DBP (11ngg ) and DEHP (64ngg ).
[Mh] Termos MeSH primário: Cromatografia Gasosa-Espectrometria de Massas/métodos
Alimentos Infantis/análise
Microextração em Fase Líquida/métodos
Ácidos Ftálicos/análise
[Mh] Termos MeSH secundário: Animais
Antracenos/análise
Galinhas
Disruptores Endócrinos/análise
Liofilização
Heptanos/química
Limite de Detecção
Carne/análise
Padrões de Referência
Solventes/química
Fatores de Tempo
Perus
Ultrassom
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthracenes); 0 (Endocrine Disruptors); 0 (Heptanes); 0 (Phthalic Acids); 0 (Solvents); 456148SDMJ (n-heptane); EH46A1TLD7 (anthracene)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170404
[Lr] Data última revisão:
170404
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170319
[St] Status:MEDLINE


  8 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
[PMID]:27615431
[Au] Autor:Huang X; Tang G; Liao Y; Zhuang X; Dong X; Liu H; Huang XJ; Ye WC; Wang Y; Shi L
[Ad] Endereço:JNU-HKUST Joint Laboratory for Neuroscience and Innovative Drug Research, Jinan University.
[Ti] Título:7-(4-Hydroxyphenyl)-1-phenyl-4E-hepten-3-one, a Diarylheptanoid from Alpinia officinarum, Protects Neurons against Amyloid-ß Induced Toxicity.
[So] Source:Biol Pharm Bull;39(12):1961-1967, 2016 Dec 01.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Amyloid-ß (Aß) is one of the major causative agents of Alzheimer's disease (AD), the most common neurodegenerative disorder characterized by progressive cognitive impairment. While effective drugs for AD are currently limited, identifying anti-Aß compounds from natural products has been shown as a promising strategy which may lead to breakthroughs for new drug candidate discovery. We have previously reported that 7-(4-hydroxyphenyl)-1-phenyl-4E-hepten-3-one (AO-1), a diarylheptanoid extracted from the plant Alpinia officinarum, has strong effects on neuronal differentiation and neurite outgrowth in vitro and in vivo. The present study further uncovers that AO-1 exerts neuroprotective effects against the neurotoxicity caused by Aß. Under the damage of Aß oligomers, the major pathological forms of Aß, dendrites of neurons become atrophic and simplified, but such impairments were substantially alleviated by AO-1 treatment. Moreover, AO-1 reduced apoptotic levels and oxidative stress triggered by Aß. Further analysis showed that the anti-caspase and dendrite protective effects of AO-1 were dependent on activation of phosphatidylinositol 3-kinase (PI3K)-mammalian target of rapamycin (mTOR) pathways. These findings collectively identify AO-1 as a beneficial compound to ameliorate the deleterious effects of Aß on dendrite integrity and cell survival, and may provide new insights on drug discovery of AD.
[Mh] Termos MeSH primário: Peptídeos beta-Amiloides/toxicidade
Heptanos/farmacologia
Fármacos Neuroprotetores/farmacologia
Fragmentos de Peptídeos/toxicidade
Fenóis/farmacologia
[Mh] Termos MeSH secundário: Alpinia
Animais
Apoptose/efeitos dos fármacos
Caspase 3/metabolismo
Células Cultivadas
Hipocampo/citologia
Neurônios/efeitos dos fármacos
Neurônios/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Fosfatidilinositol 3-Quinases/metabolismo
Ratos Sprague-Dawley
Serina-Treonina Quinases TOR/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (7-(4-hydroxyphenyl)-1-phenyl-4E-hepten-3-one); 0 (Amyloid beta-Peptides); 0 (Heptanes); 0 (Neuroprotective Agents); 0 (Peptide Fragments); 0 (Phenols); 0 (amyloid beta-protein (1-42)); EC 2.7.1.- (Phosphatidylinositol 3-Kinases); EC 2.7.1.1 (TOR Serine-Threonine Kinases); EC 2.7.1.1 (mTOR protein, rat); EC 3.4.22.- (Caspase 3)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170208
[Lr] Data última revisão:
170208
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160913
[St] Status:MEDLINE


  9 / 541 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:27565220
[Au] Autor:Cobos-Puc LE; Sánchez-López A; Centurión D
[Ad] Endereço:Departamento de Farmacobiología, Cinvestav-Coapa, Czda. de los Tenorios 235, Col. Granjas-Coapa, Deleg. Tlalpan, C.P. 14330 Ciudad de México, Mexico; Facultad de Ciencias Químicas, Universidad Autónoma de Coahuila, Boulevard Venustiano Carranza esquina con Ing. José Cárdenas Valdés, Colonia República, Saltillo, C.P. 25280 Coahuila, Mexico.
[Ti] Título:Pharmacological analysis of the cardiac sympatho-inhibitory actions of moxonidine and agmatine in pithed spontaneously hypertensive rats.
[So] Source:Eur J Pharmacol;791:25-36, 2016 Nov 15.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:This study shows that in spontaneously hypertensive rats (SHR) of 14-weeks-old, the sympathetically-induced, but not noradrenaline-induced tachycardic response are higher than age-matched Wistar normotensive rats. Furthermore, in SHR the sympathetically-induced tachycardic response was: (1) unaffected by moxonidine (3µg/kgmin); (2) partially inhibited by B-HT 933 (30µg/kgmin), both at the lowest doses; and (3) completely inhibited by the highest doses of B-HT 933 (100µg/kgmin), moxonidine (10µg/kgmin) or agmatine (1000 and 3000µg/kgmin) while the noradrenaline-induced tachycardic responses remained unaffected by the above compounds, except by 3000µg/kgmin agmatine. In SHR, 300µg/kg rauwolscine failed to block the sympatho-inhibition to 100µg/kgmin B-HT 933 or 10µg/kgmin moxonidine, but 1000µg/kg rauwolscine abolished, partially antagonized, and did not modify the sympatho-inhibition to the highest doses of B-HT 933, moxonidine, and agmatine, respectively, 3000µg/kg AGN 192403 or 300µg/kg BU224 given alone had no effect in the moxonidine- or agmatine-induced sympatho-inhibition, and the combination rauwolscine plus AGN 192403 but not plus BU224, abolished the sympatho-inhibition to the highest doses of moxonidine and agmatine. In conclusion, the sympathetically-induced tachycardic responses in SHR are inhibited by moxonidine and agmatine. The inhibition of moxonidine is mainly mediated by prejunctional α -adrenoceptors and to a lesser extent by I -imidazoline receptors, while the inhibition of agmatine is mediated by prejunctional α -adrenoceptors and I -imidazoline receptors at the same extent. Notwithstanding, the inhibitory function of α -adrenoceptors seems to be altered in SHR compared with Wistar normotensive rats.
[Mh] Termos MeSH primário: Agmatina/farmacologia
Coração/efeitos dos fármacos
Coração/inervação
Imidazóis/farmacologia
Sistema Nervoso Simpático/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Compostos Bicíclicos com Pontes/farmacologia
Coração/fisiopatologia
Frequência Cardíaca/efeitos dos fármacos
Hemodinâmica/efeitos dos fármacos
Heptanos/farmacologia
Masculino
Norepinefrina/farmacologia
Ratos
Ratos Endogâmicos SHR
Ratos Wistar
Sistema Nervoso Simpático/fisiopatologia
Ioimbina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (AGN 192403); 0 (BU 224); 0 (Bridged Bicyclo Compounds); 0 (Heptanes); 0 (Imidazoles); 2Y49VWD90Q (Yohimbine); 70J407ZL5Q (Agmatine); CC6X0L40GW (moxonidine); X4W3ENH1CV (Norepinephrine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170821
[Lr] Data última revisão:
170821
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160828
[St] Status:MEDLINE


  10 / 541 MEDLINE  
              first record previous record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:27564135
[Au] Autor:Micheli F; Bacchi A; Braggio S; Castelletti L; Cavallini P; Cavanni P; Cremonesi S; Dal Cin M; Feriani A; Gehanne S; Kajbaf M; Marchió L; Nola S; Oliosi B; Pellacani A; Perdonà E; Sava A; Semeraro T; Tarsi L; Tomelleri S; Wong A; Visentini F; Zonzini L; Heidbreder C
[Ad] Endereço:Aptuit s.r.l. , Via Fleming 4, 37135 Verona, Italy.
[Ti] Título:1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.
[So] Source:J Med Chem;59(18):8549-76, 2016 Sep 22.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of these compounds also have high selectivity over the hERG channel and were characterized with respect to their pharmacokinetic properties both in vitro and in vivo during lead identification and early lead optimization phases. A few derivatives with overall favorable developability characteristics were selected for further late lead optimization studies.
[Mh] Termos MeSH primário: Heptanos/química
Heptanos/farmacologia
Receptores de Dopamina D3/antagonistas & inibidores
Compostos de Espiro/química
Compostos de Espiro/farmacologia
[Mh] Termos MeSH secundário: Animais
Células CHO
Cricetulus
Cristalografia por Raios X
Canais de Potássio Éter-A-Go-Go/metabolismo
Seres Humanos
Modelos Moleculares
Receptores de Dopamina D3/metabolismo
Relação Estrutura-Atividade
Triazóis/química
Triazóis/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ether-A-Go-Go Potassium Channels); 0 (Heptanes); 0 (Receptors, Dopamine D3); 0 (Spiro Compounds); 0 (Triazoles)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170612
[Lr] Data última revisão:
170612
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160827
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.6b00972



página 1 de 55 ir para página                         
   


Refinar a pesquisa
  Base de dados : MEDLINE Formulário avançado   

    Pesquisar no campo  
1  
2
3
 
           



Search engine: iAH v2.6 powered by WWWISIS

BIREME/OPAS/OMS - Centro Latino-Americano e do Caribe de Informação em Ciências da Saúde