Search results for "Carini"
showing 10 items of 287 documents
Safety of tiotropium and olodaterol fixed-dose combination for COPD in patients on β-blockers
2015
Introduction: The TONADO studies (NCT01431274; NCT01431287) established the efficacy and safety of a new once-daily fixed-dose combination (FDC) with tiotropium (T), a long-acting muscarinic antagonist, and olodaterol (O), a long-acting β 2 -agonist, for the treatment of COPD. This post hoc analysis evaluates T+O safety in the subgroup of patients (pts) receiving β-blockers (BBs) in these studies. Methods: These were randomised, double-blind, parallel-group, 52-week, Phase III trials comparing T+O FDC (2.5/5 µg; 5/5 µg) with the monocomponents. Adverse events (AEs) and serious AEs (SAEs) were recorded and SAEs independently adjudicated. Pooled safety data from pts receiving BBs at baseline …
Temporal resolution and temporal transfer properties: gabaergic and cholinergic mechanisms.
2007
Temporal resolution is a basic property of the visual system and critically depends upon retinal temporal coding properties which are also of importance for directional coding. Whether the temporal coding properties for directional coding derive form inherent properties or critically depend upon the temporal coding mechanisms is unclear. Here, the influence of acetylcholine and GABA upon photopic temporal coding was investigated in goldfish, using flicker stimuli, in a behavioral and an electrophysiological (ERG) approach. The goldfish temporal resolution ability decreased from more than 90% correct choices at 20 Hz flicker frequency to about 65% at 45 Hz flicker frequency with a flicker fu…
Tiotropium in asthma: Back to the future of anticholinergic treatment
2017
Abstract Asthma is among the most common chronic diseases worldwide; however, despite progresses in the understanding of the patho-physiological mechanisms and advances in the development of new therapeutic options and strategies, the disease remains uncontrolled in a not trivial proportion of subjects. Thus, the need of new molecules to treat the underlying biological and functional abnormalities and to control symptoms is strongly advocated by clinicians. In this scenario, the most recent GINA guidelines have included the use of tiotropium bromide in the most severe and uncontrolled forms of the disease, in addition to treatment with inhaled corticosteroid plus long acting beta adrenergic…
ChemInform Abstract: Regioisomeric 5(3)-Aminomethyl-3(5)-phenylisoxazoles: Synthesis, Spectroscopic Discrimination, and Muscarinic Activity.
2010
The regioselective synthesis of isomeric 5(3)-aminomethyl-3(5)-phenyl isoxazoles using different methods is described. Spectroscopic data, especially mass spectrometric fragmentation, were used to identify and characterize the regioisomers. The muscarinic activity of these isoxazoles was assayed on isolated guinea-pig ileum and atria as well as on isolated rabbit vas deferens. Regioisomere 5(3)-Aminomethyl-3(5)-phenyl-isoxazole: Synthese, spektroskopische Unterscheidung und muskarinische Aktivitat Es werden verschiedene Verfahren zur regioselektiven Darstellung von 5(3)-Aminomethyl-3(5)-phenyl-isoxazolen beschrieben, die anhand ihrer spektroskopischen Daten, insbesondere der massenspektrosk…
Long-Term Management of Overactive Bladder with Antimuscarinic Agents
2007
Abstract Antimuscarinic therapy is the primary treatment for overactive bladder. Long-term persistence with the therapy can be problematical, and has been linked to both efficacy and tolerability. A number of specific contributory factors to poor persistence can be identified, such as adverse effects of medication, insufficient beneficial effects, inadequate follow-up after initiation of therapy (poor motivation), and unmet or unrealistic expectations (poor communication between the patient and physician). Open-label studies on antimuscarinics overestimate the real-life persistence, which can lead to unrealistic expectations of the physician. Dose flexibility has improved patient compliance…
Altered receptor binding densities in experimental antiphospholipid syndrome despite only moderately enhanced autoantibody levels and absence of beha…
2013
Abstract Experimental antiphospholipid syndrome (eAPS) in Balb/c mice causes neuropsychiatric abnormalities including hyperactivity, increased explorative behavior and cognitive deficits. Recently, we have demonstrated that these behavioral changes were linked to an upregulation of serotonergic 5-HT1A receptor binding densities in cortical and hippocampal regions while excitatory and inhibitory neurotransmitter receptors remain largely unchanged. To examine whether the observed behavioral features depend on a critical antibody concentration, mice with only moderately enhanced antiphospholipid antibodies (aPL), about 50–80% of high levels, were analyzed and compared to controls. The staircas…
Mucosa-dependent muscarinic liberation of prostaglandins from rat isolated trachea.
1995
1. The present study examined whether cholinoceptor stimulation modulates the release of arachidonic acid-derived mediators from rat isolate tracheae. 2. Tracheae were preincubated with [3H]-arachidonic acid and the outflow of 3H-compounds was determined. Acetylcholine and the muscarinic agonist, carbachol but not nicotine, increased the rate of tritium outflow maximally by about 30%. The M3 receptor-preferring antagonist rho-fluoro-hexahydrosiladiphenidol was more effective than pirenzepine and methoctramine in antagonizing the effect of acetylcholine. 3. High performance liquid chromatography analysis (methanol gradient) of the released 3H-compounds showed that one peak, co-eluting with […
Pre- and postsynaptic effects of muscarinic agonists in the guinea-pig ileum
1980
The effects of several muscarinic agonists on smooth muscle (postsynaptic effect) and on acetylcholine release (presynaptic effect) were compared in the longitudinal muscle-myenteric plexus preparation of the guinea-pig ileum. 1. For release experiments the acetylcholine stores of the preparation were labelled with 3H-choline. Electrical field stimulation in the absence of a cholinesterase inhibitor caused an outflow of tritium that reflected release of 3H-acetylcholine. The agonists oxotremorine, arecaidinepropargylester, methylfurmethide, muscarine, carbachol, arecoline and pilocarpine inhibited the stimulation-induced outflow in a concentration-dependent manner. At the highest concentrat…
Compensatory mechanisms enhance hippocampal acetylcholine release in transgenic mice expressing human acetylcholinesterase
2001
Central cholinergic neurotransmission was studied in learning-impaired transgenic mice expressing human acetylcholinesterase (hAChE-Tg). Total catalytic activity of AChE was approximately twofold higher in synaptosomes from hippocampus, striatum and cortex of hAChE-Tg mice as compared with controls (FVB/N mice). Extracellular acetylcholine (ACh) levels in the hippocampus, monitored by microdialysis in the absence or presence of 10(-8)-10(-3) M neostigmine in the perfusion fluid, were indistinguishable in freely moving control and hAChE-Tg mice. Muscarinic receptor functions were unchanged as indicated by similar effects of scopolamine on ACh release and of carbachol on inositol phosphate fo…
The release of choline from phospholipids mediated by beta-adrenoceptor activation in isolated hearts.
1986
The resting efflux of choline into the perfusate (Tyrode's solution) of isolated hearts was equal to the rate, at which choline was liberated from phospholipid degradation (Lindmar et al. 1986). Infusion of isoprenaline (2 X 10(-7) mol/l), forskolin (1-3 X 10(-6) mol/l) or 3-isobutyl-1-methylxanthine (IBMX; 3 X 10(-4) mol/l) for 40 min markedly enhanced the efflux of choline. The increase was linear during the experimental period and, in the case of isoprenaline, was blocked by 3 X 10(-7) mol/l atenolol. In the guinea-pig heart, IBMX at a threshold concentration of 10(-4) mol/l shifted the concentration-response curve for the effect of forskolin on the efflux of choline to the left by one l…