Search results for "MERIS"

Improving opportunities for effective management of gastro-oesophageal reflux disease

2002

The recent introduction of proton pump inhibitors has extraordinarily improved the therapeutic approach to gastro-oesophageal reflux disease. The concept of decreasing gastric acid secretion and increasing the pH in the lower oesophagus has been demonstrated to be therapeutically effective and the higher the level of pH achieved, the better the results. In spite of the evident efficacy of these molecules, there are still many patients who will continue to have symptoms despite medical treatment. Proton pump inhibitors suppress gastric acidity, but this effect shows a remarkable interindividual variation depending on different reasons. Thus, it is still possible to optimise medical therapy f…

Cromakalim inhibits electrically-evoked [3H]acetylcholine release from a tube-preparation of the rat isolated trachea by an epithelium-dependent mech…

1993

Rat isolated tracheae were labelled by incubation with [3H]choline to measure the tritium efflux elicited by electrical stimulation of the extrinsic parasympathetic nerves in vitro. Stimulated tritium efflux reflects the neuronal release of newly synthesized acetylcholine; the effects of potassium channel openers on the stimulated tritium efflux were investigated. In tracheae opened longitudinally neither cromakalim nor its 3S,4R-enantiomer, BRL 38227, reduced the stimulated tritium efflux, whereas in intact tube-preparations cromakalim (0.01-1 mumol/l) mediated a concentration-dependent inhibition. The inhibitory effect of 1 mumol/l cromakalim was prevented by 0.1 mumol/l glibenclamide. Li…

Pharmacokinetic evaluation of esomeprazole for the treatment of gastroesophageal reflux disease

2014

Proton pump inhibitors (PPIs) are widely used for the treatment of acid-related diseases such as gastroesophageal reflux disease (GERD). They are recommended by the American College of Gastroenterology for healing erosive esophagitis (EO) and as long-term treatment in patients with healed EO. The available PPIs differ somewhat in their pharmacokinetics and clinical properties, but whether these differences are of clinical relevance is a matter of debate. Some safety concerns have been raised with the use of PPIs, mostly an increased incidence of infectious diseases such as community-acquired pneumonia or Clostridium difficile diarrhea.This article explores the results of clinical studies on…

Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repagl…

2004

The 11 C-labeled sulfonylurea receptor 1 (SUR1) ligand (S)-2-(( 11 C)methoxy)-4-(3-methyl-1-(2-piperidine-1-yl-phenyl)- butyl-carbamoyl)-benzoic acid (( 11 C)methoxy-repaglinide) was synthesized in an overall radiochemical yield of 35% after 55 min with a radiochemical purity higher than 99%. This compound is considered for the noninvasive investigation of the SUR1 receptor status of pancreatic b-cells by positron emission tomography (PET) in the context of type 1 and type 2 diabetes. The specific activity was 40-70 GBq/lmol. In vitro testing of the nonradioactive methoxy-repaglinide was performed to characterize the affinity for binding to the human SUR1 isoform. Methoxy-repaglinide induce…

Enantioselective determination of plasma protein binding of common amphetamine-type stimulants.

2021

Amphetamine-type stimulants (ATS) like amphetamine ('speed'), methamphetamine ('crystal meth') and 3,4-methylenedioxy-N-methylamphetamine (MDMA, 'ecstasy') represent some of the most frequently abused drugs worldwide. Another less frequently abused ATS is 4-fluoroamphetamine (4-FA). The enantiomers of these four compounds exhibit different pharmacokinetic and pharmacodynamic properties. According to the free drug theory, the pharmacological properties of a substance are dependent on its plasma protein binding (PPB). However, data on PPB of stimulant enantiomers in humans are rare or non-existent. Human plasma samples were spiked with racemic mixtures of the stimulants and subjected to ultra…

Is It Possible to Produce Certified Hazelnut Plant Material in Sicily? Identification and Recovery of Nebrodi Genetic Resources, in vitro Establishme…

2021

Eight Sicilian cultivars of hazelnut (Corylus avellanaL.), namely-Curcia, Nociara Collica, Panottara Collica, Panottara Galati Grande, Parrinara, Panottara Baratta Piccola, Enzo, and Rossa Galvagno, registered into the Italian Cultivar Register of fruit tree species in 2017 were selected from Nebrodi area and establishedin vitro. The aim of the work was to carry out the sanitation of the cultivars and get virus-free plants from the most important viral pathogen threat, theapple mosaic virus. Virus-free plant material is essential for the production of certified plants from Sicilian hazelnut cultivars, complying the CE (cat. CAC) quality and the technical standards established in 2017 for vo…

Chemoselective, Substrate-directed Fluorination of Functionalized Cyclopentane β-Amino Acids

2016

This work describes a substrate-directed fluorination of some highly functionalized cyclopentane derivatives. The cyclic products incorporating CH2 F or CHF2 moieties in their structure have been synthesized from diexo- or diendo-norbornene β-amino acids following a stereocontrolled strategy. The synthetic study was based on an oxidative transformation of the ring carbon-carbon double bond of the norbornene β-amino acids, followed by transformation of the resulted "all cis" and "trans" diformyl intermediates by fluorination with "chemodifferentiation".

New orbital ephemerides for the dipping source 4U 1323-619: Constraining the distance to the source

2016

4U 1323-619 is a low mass X-ray binary system that shows type I X-ray bursts and dips. The most accurate estimation of the orbital period is 2.941923(36) hrs and a distance from the source that is lower than 11 kpc has been proposed. We aim to obtain the orbital ephemeris, the orbital period of the system, as well as its derivative to compare the observed luminosity with that predicted by the theory of secular evolution. We took the advantage of about 26 years of X-ray data and grouped the selected observations when close in time. We folded the light curves and used the timing technique, obtaining 12 dip arrival times. We fit the delays of the dip arrival times both with a linear and a quad…

Kulutuksen asema nykynuoren elämässä

1998

Engineering of charge, biotin-binding and oligomerization of avidin : new tools for avidin-biotin technology

2002

Avidin is a tetrameric glycoprotein found in chicken egg white. Due to its remarkably high affinity for biotin, avidin has widely been used in biological and biotechnical applications in life sciences. Avidin is also a highly stable protein, maintaining its functional tetrameric structure at high temperatures, extremes of pH, and in the presence of strong denaturants. In the present study we wanted to find out whether different properties of avidin can be modified with protein engineering using rational design. We used the 3D-structure of avidin together with sequence information from various avidin-like proteins to plan these changes. Besides shedding more light on the protein chemical bas…