Search results for "Amide"
showing 10 items of 3119 documents
Acute renal insufficiency and pancreatitis in a child with atypical Henoch–Schönlein purpura: efficacy of a single dose of cyclophosphamide
2018
A 9-year-old boy with petechiae on the legs and abdominal pain was unsuccessfully treated with steroids. He was admitted to our hospital for the onset of fever, ecchymosis, and arthralgia. Skin lesions suggested vasculitis, but they were not typical of Henoch–Schönlein purpura. He showed ecchymosis of the scrotal bursa, diffusion of petechiae to the trunk and arms, vomiting, severe abdominal pain, oliguria with hyponatremia, hypoalbuminemia, low C3 levels, high levels of creatinine, blood urea nitrogen, and tubular enzymes, proteinuria, and glycosuria. The urinary sediment showed macrohaematuria, and hyaline and cellular casts. Ultrasound showed polyserositis. He was treated with intraveno…
Prostasome-like vesicles stimulate acrosome reaction of pig spermatozoa
2007
Abstract Background The presence of small membranous particles characterizes the male genital fluids of different mammalian species. The influence of semen vesicles, denominated prostasomes, on sperm functional properties has been well documented in humans, but their biological activity is scarcely known in other species. The present work investigated prostasome-like vesicles in pig semen for their ability to interact with spermatozoa and to affect acrosome reaction. Methods Prostasome-like vesicles have been isolated from pig seminal plasma by high-speed centrifugation and Sephadex G-200 gel chromatography. Morphology of purified vesicles has been checked by scanning electron microscopy wh…
Amino Acid Derivatives as Palmitoylethanolamide Prodrugs: Synthesis, In Vitro Metabolism and In Vivo Plasma Profile in Rats
2015
Palmitoylethanolamide (PEA) has antinflammatory and antinociceptive properties widely exploited in veterinary and human medicine, despite its poor pharmacokinetics. Looking for prodrugs that could progressively release PEA to maintain effective plasma concentrations, we prepared carbonates, esters and carbamates at the hydroxyl group of PEA. Chemical stability (pH 7.4) and stability in rat plasma and liver homogenate were evaluated by in vitro assays. Carbonates and carbamates resulted too labile and too resistant in plasma, respectively. Ester derivatives, prepared by conjugating PEA with various amino acids, allowed to modulate the kinetics of PEA release in plasma and stability in liver …
Phenylamides of 1-Phenyl (or Methyl)-5-benzamidopyrazole-4-carboxylic Acid as Vratizolin Analogs with Analgesic and Antiinflammatory Activities
2001
A number of phenylamides of 5-benzamidopyrazole-4-carboxylic acid were prepared in 50-80 % yields from 1-phenyl (or methyl) 6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-ones and aniline derivatives. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their ulcerogenic potential and acute toxicity. Some derivatives, when compared to phenylbutazone, proved more active in the tests for analgesie and antiexudative activities, but less active in the carrageenin paw oedema test. The compounds proved to posses marginal or no ulcerogenic effect, as well as low systemic toxicity.
Argatroban for elective percutaneous coronary intervention: The ARG-E04 multi-center study
2011
The synthetic arginine-derived direct thrombin inhibitor argatroban is an attractive anticoagulant for percutaneous coronary intervention (PCI), because of its rapid onset and offset, and its hepatic elimination. Argatroban was approved for PCI in patients with heparin-induced thrombocytopenia (HIT). However, there are limited data about argatroban in non-HIT patients. The objective of this open-label, multiple-dose, controlled study was to examine the safety and efficacy of argatroban in patients undergoing elective PCI.Of 140 patients randomized to three argatroban dose groups (ARG250, ARG300, and ARG350 with 250, 300, or 350 μg/kg bolus, followed by 15, 20, or 25 μg/kg/min infusion) and …
Treatment of Fabry Disease management with migalastat-outcome from a prospective 24 months observational multicenter study (FAMOUS).
2020
Abstract Aims Fabry disease (FD) is an X-linked lysosomal storage disorder caused by a deficiency of the lysosomal enzyme α-galactosidase A (GLA/AGAL), resulting in the lysosomal accumulation of globotriaosylceramide (Gb3). Patients with amenable GLA mutations can be treated with migalastat, an oral pharmacological chaperone increasing endogenous AGAL activity. In this prospective observational multicentre study, safety as well as cardiovascular, renal, and patient-reported outcomes and disease biomarkers were assessed after 12 and 24 months of migalastat treatment under ‘real-world’ conditions. Methods and results A total of 54 patients (26 females) (33 of these [61.1%] pre-treated with en…
Clinical manifestations of Fabry disease in children: data from the Fabry Outcome Survey.
2006
Background Fabry disease is a rare X-linked disorder caused by deficient activity of the enzyme alpha-galactosidase A. This produces progressive lysosomal accumulation of globotriaosylceramide throughout the body, leading to organ failure and premature death. Aim Here, we present the clinical manifestations of Fabry disease in children enrolled in FOS--the Fabry Outcome Survey--a European database of the natural history of Fabry disease and the effects of enzyme replacement therapy with agalsidase alfa (Replagal). Methods Currently, there are 545 patients in FOS, from 11 European countries. We analysed the baseline demographic and clinical characteristics of 82 of these patients (40 boys, 4…
Changes in myosin heavy chain composition with heavy resistance training in 60- to 75-year-old men and women.
2001
The purpose of this investigation was to assess the myosin heavy chain (MHC) expression in the vastus lateralis muscle from elderly men and women, and to determine whether heavy resistance training influences its expression. Twenty healthy, mildly physically active subjects gave their informed consent to participate in the study. The experimental group consisted of seven men and seven women [mean (SD) age 65.5 (4.1) years] and the control group consisted of three men and three women [mean (SD) age 62.3 (3.6) years]. The 6-month resistance training program was divided into two phases with weeks 1-12 consisting of high-intensity resistance training, and weeks 13-24 involving power training. M…
Nicotinic cholinoceptors in the rat pineal gland as analyzed by Western blot, light- and electron microscopy
1992
Abstract The monoclonal antibody WF6, raised against purified Torpedo nicotinic acetylcholine receptor (nAChR) was used to study the distribution of cholinoceptors in the rat pineal gland by means of Western blot analysis, light- and electron microscopy. The immunoblot analysis using homogenized pineal gland revealed a labeled protein band of apparent molecular weight 40 kDa which was identified as α-subunits of a nAChR. In the light microscope, approximately one-fourth of the pinealocytes exhibited cytoplasmic immunoreactivity (IR) of varying density. In the electron microscope, IR was seen as patchy staining of cell membranes of pinealocyte somata and processes. Presynaptic IR material wa…
Pronounced cholinergic but only moderate purinergic effects in isolated atrial and ventricular heart muscle from cats.
1989
1 The effects of cholinergic and purinergic stimulation on action potential, force of contraction and 86Rb efflux were investigated in cat atrial and/or ventricular heart muscle. 2 Acetylcholine and carbachol exerted a concentration-dependent negative inotropic effect in cat atrial heart muscle. Carbachol 10 μmol l−1 completely abolished the force of contraction and increased the rate constant of 86Rb efflux 2–3 fold, whereas the action potential duration was shortened to about 1/10 of its length under control conditions. 3 The effects of acetylcholine and carbachol in cat atrial heart muscle were mimicked, qualitatively, by adenosine and its analogues 5′-(N-ethyl)-carboxamido-adenosine (NE…