Search results for "Mimetic"
showing 10 items of 218 documents
New Fluorinated Peptidomimetics through Tandem Aza-Michael Addition to α-Trifluoromethyl Acrylamide Acceptors: Synthesis and Conformational Study in …
2009
A range of partially modified retro (PMR) psi[NHCH(2)] peptide mimetics containing a hydrolytically stable CH(2)CH(CF(3))CO unit have been synthesized. The first kind of peptidomimetics is obtained from the highly efficient aza-Michael addition of different amines to alpha-trifluoromethyl acrylamide acceptors. Subsequent deprotection of the amino group furnishes the key common intermediate for the synthesis of other families of peptidomimetics: dipeptides, tripeptides, peptidomimetics containing a urea moiety, and structures containing two units of alpha-trifluoromethyl-beta(2)-alanine. Finally, a conformational study of several of the newly synthesized peptidomimetics, performed with the a…
Highly stereoselective tandem aza-Michael addition-enolate protonation to form partially modified retropeptide mimetics incorporating a trifluoroalan…
2003
Clinical and imaging outcome of osteochondral lesions of the talus treated using autologous matrix-induced chondrogenesis technique with a biomimetic…
2017
Abstract Background The purpose of our study was to assess the clinical and imaging outcome of autologous matrix-induced chondrogenesis (AMIC) technique consisting of microfractures followed by the filling of osteochondral lesions of the talus (OLTs) with a cell-free biphasic collagen-hydroxyapatite osteochondral scaffold (MaioRegen). Methods Sixteen patients (eight males, age: 42.6 ± 18.4, range 14–74) with OLT repaired using AMIC technique, with implantation of MaioRegen, were clinically evaluated through the American Orthopedic Foot and Ankle Society Score (AOFAS) and a 10-point Visual Analogue Scale (VAS) pain score after a mean follow-up of 30 ± 16.9 months. The MRI examinations were p…
Vulnerability to psychotogenic effects of ketamine is associated with elevated D2/3-receptor availability.
2012
Previous positron emission tomography (PET) studies employing competition paradigms have shown either no change or substantial declines in striatal ( 11 C)-raclopride binding after challenge with psychotogenic doses of the N-methyl-D-aspartate antagonist ketamine. We sought to probe the relationship between the severity of ketamine-induced psychotic symptoms and altered dopamine D2/3 receptor availability throughout brain using the high affinity ligand ( 18 F)-fallypride (FP). PET recordings were obtained in a group of 10 healthy, young male volunteers, in a placebo condition, and in the course of an infusion with ketamine at a psychotomimetic dose. Administration of the Positive and Negati…
Characterization of sensory neurotransmission and its inhibition via alpha 2B-adrenoceptors and via non-alpha 2-receptors in rabbit iris.
1993
To find out whether, and which type of, adrenoceptors mediate prejunctional inhibition of sensory neurotransmitter release from trigeminal fibres, the modulation of twitch response to electrical field stimulation on rabbit isolated iris was investigated. Evoked iris sphincter contractions consisted of a minor fast cholinergic and a large slow component. The latter was unaffected by atropine and guanethidine, hence nonadrenergic noncholinergic in nature (NANC), but nearly completely abolished by capsaicin pretreatment and by the neurokinin receptor antagonist spantide. The response was probably not mediated by NK2 receptors as SR 48,968, an NK2 selective nonpeptide antagonist, failed to redu…
Synthesis of polyfluoroalkyl sp2-iminosugar glycolipids and evaluation of their immunomodulatory properties towards anti-tumor, anti-leishmanial and …
2019
Immunomodulatory glycolipids, among which α-galactosylceramide (KRN7000) is an iconic example, have shown strong therapeutic potential in a variety of conditions ranging from cancer and infection to autoimmune or neurodegenerative diseases. A main difficulty for those channels is that they often provoke a cytokine storm comprising both pro- and anti-inflammatory mediators that antagonize each other and negatively affect the immune response. The synthesis of analogues with narrower cytokine secretion-inducing capabilities is hampered by the intrinsic difficulty at controlling the stereochemical outcome in glycosidation reactions, particularly if targeting the α-anomer, which seriously hamper…
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…
Implementation of IFRS in Japan: An Analysis of Voluntary Adoption by Listed Firms
2019
Since 2010 Japanese listed firms can voluntarily use international financial reporting standards for their consolidated financial statements. Using financial and non-financial data, we carry out a comprehensive research into the adopters’ determinants. We employ a multi-period logit model that considers every annual decision made along the period 2010-2019. We find that the having outside networks through subsidiaries and a strong internal corporate governance system are key factors. We also confirm a contagion effect. Finally, our results suggest that goodwill is also relevant, since only Japanese accounting standards require annual amortization.
Calculation of the pH and the titratable acidity in clinically used infusion solutions.
2006
Clinically used infusion solutions are complex aqueous mixtures composed of a variety of different salts, acids, and non-electrolytes, and are characterized by composition, initial pH, and titratable acidity (TA). By rigorous treatment as a multi-composed acid-base system, pH and TA were calculated from proton dissociation equilibria, mass balance equations and electroneutrality condition. Nine were arbitrarily chosen as model solutions in which pH and TA were experimentally determined. From composition, and based on a set of apparent acidity constants (pK values) at 37 degrees C and total ionic strength 0.155 mol/l, pH was calculated by iteration. In the model solutions, measured pH was in…
FIctional Artworks. Literary Ékphrasis and the Invention of Images
2016
The volume is devoted to images in painting, photography and cinema invented by literature. At the same time it intends to question, through this perspective, the relationship between text and image, between verbal and visual in modern and contemporary literature. The authors investigate the mutual boundaries between literature and arts from the point of view of aesthetics, visual culture and literary theory, trying to build a map of the notional ékphrasis, a description which constitutes the work of art while telling it.