Search results for "ECL"
showing 10 items of 1262 documents
Preclinical evidence of new opioid modulators for the treatment of addiction.
2010
Addiction to opiates is one of the most severe forms of substance dependence, and despite a variety of pharmacological approaches to treat it, relapse is observed in a high percentage of subjects. New pharmacological compounds are necessary to improve the outcome of treatments and reduce adverse side effects. Moreover, drugs that act on the opioid system can also be of benefit in the treatment of alcohol or cocaine addiction. AREA COVERED BY THIS REVIEW: Recent preclinical studies of pharmacological agents for the treatment of opiate addiction (2008 to the present date).The reader will be informed of the latest drugs shown in animal models to modify dependence on opiates and the reinforcing…
Covalent binding of drug metabolites to DNA ? a tool of predictive value?
1980
The presently available data suggest at least some correlation between covalent binding of drug metabolites to DNA and carcinogenicity of that drug. More data, however, are needed to establish the predictability of covalent DNA binding assays for extrahepatic cancer. A covalent binding assay requires administration of radioactively labelled compound to the experimental animals; the availability of labelled compound and requirements as to radiochemical purity, chemical and biochemical stability are limiting the applicability of this procedure. Many technical pitfalls accompany covalent DNA binding assays. It is concluded that at the present time DNA binding assays do not represent routine pr…
Lung deposition of extrafine inhaled corticosteroid (ICS)-containing fixed combinations drug in COPD patients using Functional Respiratory Imaging (F…
2018
Introduction: FRI is a novel computational fluid dynamics (CFD)-based technique using formulation profile and patients lung CT scan to simulate aerosol deposition. Aims and objectives: To evaluate lung deposition of pressurized metered dose inhaler (pMDI) extrafine beclometasone dipropionate/formoterol fumarate/glycopyrronium (BDP/FF/G Trimbow®) with pMDI extrafine BDP/FF (Foster®) pMDI and compared them with reference gamma scintigraphy data. Methods: FRI was used to assess, in silico, the deposition of pMDI combination products (BDP/FF/G and BDP/FF) in 20 moderate to severe COPD patients. FRI combined high-resolution lung CT scans of each patient with in silico computational flow simulati…
Inkjet printing methodologies for drug screening
2010
We show for the first time a contactless, low-cost, and rapid drug screening methodology by employing inkjet printing for molecular dispensing in a microarray format. Picoliter drops containing a model substrate (D-glucose)/ inhibitor (D-glucal) couple were accurately dispensed on a single layer consisting of the enzymatic target (glucose oxidase) covalently linked to a functionalized silicon oxide support. A simple colorimetric detection method allowed one to prove the screening capability of the microarray with the possibility to assay with high reproducibility at the single spot level. Measurements of the optical signal as a function of concentration and of time verified the occurrence a…
Targeting apoptosis in solid tumors: the role of bortezomib from preclinical to clinical evidence.
2007
The ubiquitin-proteasome pathway is the main proteolytic system present in the nucleus and cytoplasm of all eukaryotic cells. Apoptosis activation induced by ubiquitin-proteasome pathway inhibition makes the proteasome a new target of anticancer therapy. Bortezomib is the first proteasome inhibitor to be approved by the US FDA; in 2003 as a third line and in 2005 as a second line therapy for the treatment of multiple myeloma only. This review focuses on the use of bortezomib, not only in its therapeutic role but also, more specifically, in its biologic role and discusses the most recent applications of the drug in solid tumors, both at a preclinical and clinical level.
Cell Lines: A Tool for In Vitro Drug Metabolism Studies
2008
Primary cultured hepatocytes are a valuable in vitro model for drug metabolism studies. However, their widespread use is greatly hindered by the scarcity of suitable human liver samples. Moreover, the well-known in vitro phenotypic instability of hepatocytes, the irregular availability of fresh human liver for cell harvesting purposes, and the high batch-to-batch functional variability of hepatocyte preparations obtained from different human liver donors, seriously complicate their use in routine testing. To overcome these limitations, different cell line models have been proposed for drug metabolism screening. Human liver-derived cell lines would be ideal models for this purpose given thei…
Cognitive Frailty: An Update
2021
This review article provides an update of the empirical research on cognitive fragility conducted in the last four years. The studies retrieved were classified in four different categories. The first category includes articles relating cognitive frailty to cognitive reserve and which continue to highlight the importance of educational level. The second category includes recent research on cognitive fragility biomarkers, involving neuroimaging, metabolism and, in a novel way, microbiota. The third category includes research on how cognitive frailty is related to motor development and physical functioning, exploring e.g. the use of technology to study motor markers of cognitive frailty. Final…
DIDÁCTICA DE LAS ARTES CON TIC, APRENDIZAJE COLABORATIVO E INTERDISCIPLINARIEDAD EN LA FORMACIÓN INICIAL DEL PROFESORADO
2021
El aprendizaje mediante las tecnologías de la información y comunicación y la interdisciplinariedad como ejes de la innovación pedagógica son aspectos que se deben fomentar en la Educación Superior desde la declaración de Bolonia, hace ya veinte años. Sin embargo, todavía no han arraigado lo suficiente en muchas aulas universitarias. Es por ello que se presenta un estudio sobre una experiencia educativa desarrollada por profesorado de las áreas de didáctica de la expresión musical, plástica y corporal con futuros docentes en formación. Los objetivos son promover el uso de las TIC, nuevos sistemas de comunicación de los trabajos académicos y el aprendizaje colaborativo e interdisciplinar ent…
Early handling effect on female rat spatial and non-spatial learning and memory
2014
This study aims at providing an insight into early handling procedures on learning and memory performance in adult female rats. Early handling procedures were started on post-natal day 2 until 21, and consisted in 15 min, daily separations of the dams from their litters. Assessment of declarative memory was carried out in the novel-object recognition task; spatial learning, reference- and working memory were evaluated in the Morris water maze (MWM). Our results indicate that early handling induced an enhancement in: (1) declarative memory, in the object recognition task, both at 1h and 24h intervals; (2) reference memory in the probe test and working memory and behavioral flexibility in the…
Two atropisomers of tricarbonyl[η6-7-chloro-3-(3-chloro-2-methylphenyl)-2,4,8-trimethyl-1,2,3,4-tetrahydro-2,4-dibora-1,3-diazanaphthalene]chromium(0)
2001
The structures of two atropisomers of the title compound, [Cr(C16H18B2Cl2N2)(CO)3], are reported. For both compounds, the Cr(CO)3 moiety is bound to the C6 aromatic ring of the molecule; the existence of atropisomers resulting from the non-equivalence of both faces of the C6 aromatic ring is a consequence of the 3-chloro-2-methylphenyl ring being nearly perpendicular to the mean plane of the 2,4-dibora-1,3-diazanaphthalene ring. The orientation of the Cr(CO)3 tripod relative to the C6 aromatic ring is such that it is nearly eclipsed in one isomer (2.4° rotation from being eclipsed with C—N, C—Cl and C—H) and slightly twisted (16.2°) from an eclipsed conformation in the other.