Search results for "IPR"
showing 10 items of 1515 documents
Farmaceitisko vielu ekotoksiskuma riska novērtējums uz mikroorganismiem notekūdeņos
2017
Vides piesārņojums ar AFV šobrīd ir aktuāla problēma un ir nepieciešamas zināšanas par iespējamajām šī piesārņojuma sekām. Darba mērķis bija pētīt baktēriju P.fluorescens AM 11 un M.luteus fizioloģiskās atbildes reakciju uz dažādu farmaceitisko vielu klātbūtni, kā arī novērtēt kā paaugstinātas ibuprofēna koncentrācijas ietekmē aktīvo dūņu baktēriju sabiedrības daudzveidību un antibiotiku rezistences veidošanos. Antibiotika ciprofloksacīns uzrāda visspēcīgāko inhibējošo efektu uz P.fluorescens AM 11 un M.luteus baktēriju kultūrām periodiskā kultūrā mikroplatēs. Augstas ibuprofēna koncentrācijas aktīvajāss dūņās veicina Sphingomonadales un Enterobacteriales kārtas baktēriju attīstību un uzrād…
Failed Total Hip Arthroplasty: Diagnostic Performance of Conventional MRI Features and Locoregional Lymphadenopathy to Identify Infected Implants.
2020
Background Very little has been published about the diagnostic performance of MRI in total hip arthroplasty (THA) infection. Purpose To determine the diagnostic performance of conventional MRI features and of new lymph nodal indices to identify infection in patients with failed THA. Study type Retrospective. Population In all, 119 patients (66 females; age 66.9 ± 12.4 years) with failed THA. Field strength/sequences Metal artifact reduction sequence (MARS) protocol including short tau inversion recovery and turbo spin-echo T1 - and T2 -weighted sequences at 1.5T. Assessment Patients underwent pelvis MRI prior to failed THA revision. MRIs were reviewed to identify periprosthetic bone destruc…
Comparative study on the inhibition of Na+, K+-activated ATPase activity by chlorpromazine, promazine, imipramine, and their monodesmethyl metabolites
1972
The inhibition of the sodium- and potassium-activated adenosine triphosphatase (Na-K-ATPase, EC 3.6.1.3) activity by chlorpromazine, promazine and imipramine was compared with that by the monodesmethyl metabolites of these drugs. The experiments were performed with a deoxycholate- and sodium iodide-treated microsomal enzyme preparation from rat brain. It was shown in dose-response curves as well as in double-reciprocal Lineweaver-Burk plots of Na-K-ATPase activity against KCl concentration that the monodesmethyl metabolites were stronger inhibitors than their parent compounds. The results obtained with the desmethyl metabolites and imipramine as inhibitors indicate competitive inhibition wh…
Automated Determination of Paroxetine and Its Main Metabolite by Column Switching and On-Line High-Performance Liquid Chromatography
1994
An automated column-switching method coupled to isocratic high-performance liquid chromatography has been developed for simultaneous determination of blood levels of paroxetine and its nonconjugated main metabolite BRL 36610. The lower limits of detection were 9-15 nmol/L (3-5 ng/ml) and linearity between drug concentration and detector response was found for 0-1,500 nmol/L (0-500 ng/ml). The method could be applied to the analysis of serum samples obtained from depressed patients who were treated with daily oral doses of 20 or 40 mg of paroxetine. After the 20-mg dose, the mean blood level of paroxetine was 69 nM (23 ng/ml), whereas the metabolite BRL 36610 was detectable in only one of 5 …
Neurotrophic Properties of Silexan, an Essential Oil from the Flowers of Lavender-Preclinical Evidence for Antidepressant-Like Properties.
2020
Abstract Background Silexan, a special essential oil from flowering tops of lavandula angustifolia, is used to treat subsyndromal anxiety disorders. In a recent clinical trial, Silexan also showed antidepressant effects in patients suffering from mixed anxiety-depression (ICD-10 F41.2). Since preclinical data explaining antidepressant properties of Silexan are missing, we decided to investigate if Silexan also shows antidepressant-like effects in vitro as well as in vivo models. Methods We used the forced swimming test (FST) in rats as a simple behavioral test indicative of antidepressant activity in vivo. As environmental events and other risk factors contribute to depression through conve…
Low Density Lipoprotein Receptor-related Protein (LRP) Interacts with Presenilin 1 and Is a Competitive Substrate of the Amyloid Precursor Protein (A…
2005
Presenilin 1 (PS1) is a critical component of the gamma-secretase complex, which is involved in the cleavage of several substrates including the amyloid precursor protein (APP) and the Notch receptor. Recently, the low density receptor-related protein (LRP) has been shown to be cleaved by a gamma-secretase-like activity. We postulated that LRP may interact with PS1 and tested its role as a competitive substrate for gamma-secretase. In this report we show that LRP colocalizes and interacts with endogenous PS1 using coimmunoprecipitation and fluorescence lifetime imaging microscopy. In addition, we found that gamma-secretase active site inhibitors do not disrupt the interaction between LRP an…
Usi pubblici e politici di Dante Alighieri
2022
The commemorations of Dante Alighieri ‘s 700th death anniversary saw in 2021 a ‘national’ and even a ‘nationalist ‘ Dante cropping up once again in the Italian public discourse. This article summarises the history of the public and political uses of the poet of the Divina Commedia: from the end of the 18th century, when his modern cult was born, to the Risorgimento, from the First World War to Fascism, up to the more recent ‘pop’ Dante.
High-throughput screening with the Eimeria tenella CDC2-related kinase2/cyclin complex EtCRK2/EtCYC3a
2012
The poultry disease coccidiosis, caused by infection with Eimeria spp. apicomplexan parasites, is responsible for enormous economic losses to the global poultry industry. The rapid increase of resistance to therapeutic agents, as well as the expense of vaccination with live attenuated vaccines, requires the development of new effective treatments for coccidiosis. Because of their key regulatory function in the eukaryotic cell cycle, cyclin-dependent kinases (CDKs) are prominent drug targets. The Eimeria tenella CDC2-related kinase 2 (EtCRK2) is a validated drug target that can be activated in vitro by the CDK activator XlRINGO (Xenopus laevis rapid inducer of G2/M progression in oocytes). B…
In situ kinetic modelling of intestinal efflux in rats: functional characterization of segmental differences and correlation with in vitro results.
2007
The objective was to devise and apply a novel modelling approach to combine segmental in situ rat perfusion data and in vitro cell culture data, in order to elucidate the contribution of efflux in drug absorption kinetics. The fluoroquinolone CNV97100 was used as a model P-gp substrate. In situ intestinal perfusion was performed in rat duodenum, jejunum, ileum and colon to measure the influence of P-gp expression on efflux. Inhibition studies of CNV97100 were performed in the presence of verapamil, quinidine, cyclosporin A and p-aminohippuric acid. Absorption/efflux parameters were modelled simultaneously, using data from both in situ studies as well as in vitro studies. The maximal efflux …
Convenient synthesis of pyrrolo[3,4-g]indazole
2013
Abstract The synthesis of a novel class of tetrahydropyrrolo[3,4-g]indazoles is reported, by annelation of the pyrazole ring on the isoindole moiety by means of 5-hydroxymethylene tetrahydroisoindole-4-ones key intermediates, with good regioselectivity. Dihydroderivatives were also obtained by oxidation with DDQ of the corresponding tetrahydropyrrolo[3,4-g]indazoles. The growth inhibitory effect was evaluated at the National Cancer Institute of Bethesda and some derivatives showed modest activity.