Search results for "Ethanolamine"
showing 10 items of 122 documents
Design, Synthesis, and Biological Evaluation of Novel Fluorinated Ethanolamines
2011
The preparation of novel fluorinated allylamines and their use as key fragments for the stereoselective synthesis of hydroxyethyl secondary amine (HEA)-type peptidomimetics is described. Our strategy employs chiral sulfinyl imines as synthesis intermediates, by treatment of hemiaminal precursors with two equivalents of vinylmagnesium bromide. The subsequent oxidation of the allylic amines to the corresponding epoxides was achieved by treatment with methyl(trifluoromethyl)dioxirane. Finally, epoxide ring opening with a range of nitrogen nucleophiles provided a library of HEA-derived peptidomimetics with a phenyldifluoromethylene moiety. The biological evaluation of these derivatives revealed…
Development and validation of a liquid chromatography tandem mass spectrometry method for the analysis of beta-agonists in animal feed and drinking w…
2010
A reproducible, sensitive and selective multiresidue analytical method for seven beta-agonists: clenbuterol (CBT), clenpenterol (CPT), ractopamine (RTP), brombuterol (BBT), mabuterol (MBT), mapenterol (MPT), and hydroxymethylclenbuterol (HMCBT) was developed and validated by using liquid chromatography tandem mass spectrometry (LC-MS/MS) in feed and drinking water samples. The validation was achieved according to the criteria laid down in the Commission Decision 2002/657/EC, however it was necessary to use minimum required performance limits (MRPLs) proposed by the Community Reference Laboratories (CRLs) due to the lack of maximum residue limits (MRLs) for beta-agonists. By setting up these…
Pharmacological blockade of the fatty acid amide hydrolase (FAAH) alters neural proliferation, apoptosis and gliosis in the rat hippocampus, hypothal…
2015
Endocannabinoids participate in the control of neurogenesis, neural cell death and gliosis. The pharmacological effect of the fatty acid amide hydrolase (FAAH) inhibitor URB597, which limits the endocannabinoid degradation, was investigated in the present study. Cell proliferation (phospho-H3(+) or BrdU(+) cells) of the main adult neurogenic zones as well as apoptosis (cleaved caspase-3(+)), astroglia (GFAP(+)), and microglia (Iba1(+) cells) were analyzed in the hippocampus, hypothalamus and striatum of rats intraperitoneally treated with URB597 (0.3 mg/kg/day) at one dose/4-days resting or 5 doses (1 dose/day). Repeated URB597 treatment increased the plasma levels of the N-acylethanolamine…
Varietal and geographic classification of french red wines in terms of elements, amino acids and aromatic alcohols
1988
Thirty-four French red wines from three regions already studied for their anthocyanin and flavonoid constituents have been further analysed for elements, amino acids and aromatic alcohols. An interpretation of the differences between wines related to their different geographic and varietal origins has been made from the results of statistical analyses: F statistic, principal component analysis (PCA) and stepwise discriminant analysis (SDA). Wine samples produced near Bordeaux were found to be characterised by higher rubidium and lower lithium and calcium concentrations. Differences between wine samples made from the same grape variety or produced in the same region are mainly related to dif…
Budesonide/formoterol maintenance and reliever therapy: a new treatment approach for adult patients with asthma.
2007
An inhaled corticosteroid (ICS) or an ICS/long-acting beta(2)-agonist (LABA) combination plus short-acting beta(2)-agonist (SABA) as needed for symptom relief is recommended for persistent asthma. Additionally, budesonide/formoterol maintenance and reliever therapy (Symbicort SMART, AstraZeneca, Sweden) has been approved for adults in the European Union. This option is well tolerated and offers greater reductions in asthma exacerbations together with similar improvements in daily symptom control, at a lower overall steroid load, compared with fixed-dose ICS/LABA plus SABA.Two large clinical trials investigated the use of budesonide/formoterol as maintenance and reliever compared with medium…
Overall asthma control: the relationship between current control and future risk.
2009
Background Asthma guidelines emphasize both maintaining current control and reducing future risk, but the relationship between these 2 targets is not well understood. Objective This retrospective analysis of 5 budesonide/formoterol maintenance and reliever therapy (Symbicort SMART Turbuhaler ∗ ∗Symbicort SMART and Turbuhaler are trademarks owned by AstraZeneca. Neither the Symbicort SMART posology nor the dry powder formulation Turbuhaler are currently approved in the United States.) studies assessed the relationship between asthma control questionnaire (ACQ-5) and Global Initiative for Asthma-defined clinical asthma control and future risk of instability and exacerbations. Methods The perc…
Th17 immunity in children with allergic asthma and rhinitis: a pharmacological approach
2013
Th17 cells and IL-17A play a role in the development and progression of allergic diseases. We analyzed the IL-17A levels in sputum supernatants (Ss), nasal wash (NW) and plasma (P) from Healthy Controls (HC) and children with Asthma/Rhinitis. We tested the expression of IL-17A, RORγ(t) and FOXP3 in peripheral blood T-lymphocytes from intermittent and mild-moderate asthma. The effect of Budesonide and Formoterol was tested "in vitro" on IL-17A, RORγ(t) and FOXP3 expression in cultured T-lymphocytes from mild-moderate asthma/persistent rhinitis patients, and on nasal and bronchial epithelial cells stimulated with NW and Ss from mild-moderate asthma/persistent rhinitis. Further, the effect of …
Budesonide/formoterol for the treatment of asthma.
2003
Budesonide/formoterol (Symbicort), AstraZeneca plc) is a novel treatment for asthma, combining an inhaled corticosteroid - budesonide, and a long-acting beta(2)-agonist - formoterol, in a single inhaler, the Turbuhaler. Randomised, clinical studies in patients with asthma have demonstrated that budesonide/formoterol is more effective than the inhaled corticosteroids, budesonide and fluticasone alone, and at least as effective as both monocomponents in separate inhalers. Results from clinical studies suggest a synergistic effect when both drugs are administered via one inhaler, although the mechanisms for this are not fully understood. Budesonide/formoterol has a rapid onset of effect, appar…
Budesonide/formoterol for maintenance and reliever therapy in the management of moderate to severe asthma.
2008
The Global Initiative for Asthma (GINA) guidelines aim at improving asthma control and preventing future risk. For patients with moderate to severe asthma an inhaled corticosteroid (ICS) or an ICS/long-acting beta2-agonist (LABA) combination with a short-acting beta2-agonist (SABA) as reliever is recommended. Despite the availability of effective maintenance therapies, a large proportion of patients still fail to achieve guideline-defined asthma control, and overuse of SABA reliever medication at the expense of ICS is commonly observed. New simplified treatment approaches may offer a solution and assist physicians to achieve overall asthma control. One such treatment approach, which is reco…
Patterns of Innate or Acquired Resistance to Anticancer Drugs: Our Experience to Overcome It
2021
Drug resistance, which is often of a multiple type, can be defined as the ability of cancer cells to obtain resistance to both conventional and novel chemotherapy agents. It remains a major problem to solve in cancer therapy. The mechanisms of resistance are multifactorial, and in our cellular models of acute myeloid leukemia, hepatocellular carcinoma, and triple-negative breast cancer, it involves the NF-κB pathway. In our opinion, multitarget molecules can be considered as privileged compounds capable of attacking and reversing the resistant phenotype. In the phenomena of both innate and acquired drug resistance that we have been studying since 1998 to today and up to 2016 under the guida…