Search results for "lazine"
showing 10 items of 75 documents
AMG900 as novel inhibitor of the translationally controlled tumor protein
2020
Abstract Introduction Cancer is one of the leading causes of death worldwide. Classical cytotoxic chemotherapy exerts high side effects and low tumor selectivity. Translationally controlled tumor protein (TCTP) is a target for differentiation therapy, a promising, new therapeutic approach, which is expected to be more selective and less toxic than cytotoxic chemotherapy. The aim of the present investigation was to identify novel TCTP inhibitors. Methods We performed in silico screening and molecular docking using a chemical library of more than 31,000 compounds to identify a novel inhibitor of TCTP. We tested AMG900 in vitro for binding to TCTP by microscale thermophoresis and co-immunoprec…
Effects of Ranolazine on Astrocytes and Neurons in Primary Culture.
2016
Ranolazine (Rn) is an antianginal agent used for the treatment of chronic angina pectoris when angina is not adequately controlled by other drugs. Rn also acts in the central nervous system and it has been proposed for the treatment of pain and epileptic disorders. Under the hypothesis that ranolazine could act as a neuroprotective drug, we studied its effects on astrocytes and neurons in primary culture. We incubated rat astrocytes and neurons in primary cultures for 24 hours with Rn (10-7, 10-6 and 10-5 M). Cell viability and proliferation were measured using trypan blue exclusion assay, MTT conversion assay and LDH release assay. Apoptosis was determined by Caspase 3 activity assay. The …
Ranolazine-Mediated Attenuation of Mechanoelectric Feedback in Atrial Myocyte Monolayers.
2020
[EN] Background Mechanical stretch increases Na(+)inflow into myocytes, related to mechanisms including stretch-activated channels or Na+/H(+)exchanger activation, involving Ca(2+)increase that leads to changes in electrophysiological properties favoring arrhythmia induction. Ranolazine is an antianginal drug with confirmed beneficial effects against cardiac arrhythmias associated with the augmentation ofI(NaL)current and Ca(2+)overload. Objective This study investigates the effects of mechanical stretch on activation patterns in atrial cell monolayers and its pharmacological response to ranolazine. Methods Confluent HL-1 cells were cultured in silicone membrane plates and were stretched to…
NEW THERAPEUTIC PERSPECTIVES IN IRRITABLE BOWEL SYNDROME: TARGETING LOW-GRADE INFLAMMATION, IMMUNO-NEUROENDOCRINE AXIS, MOTILITY, SDECRETION AND BEYO…
2017
Irritable bowel syndrome (IBS) is a chronic, recurring, and remitting functional disorder of the gastrointestinal tract characterized by abdominal pain, distention, and changes in bowel habits. Although there are several drugs for IBS, effective and approved treatments for one or more of the symptoms for various IBS subtypes are needed. Improved understanding of pathophysiological mechanisms such as the role of impaired bile acid metabolism, neurohormonal regulation, immune, dysfunction, the epithelial barrier and the secretory properties of the gut has led to advancements in the treatment of IBS. With regards to therapies for restoring intestinal permeability, multiple studies with prebiot…
Pressure-Stabilized Solvates of Xylazine Hydrochloride
2016
High pressure strongly favors the highest-density polymorph Z of active pharmaceutical ingredient 2-(2,6-xylidino)-5,6-dihydro-4H-1,3-thiazine hydrochloride (xylazine hydrochloride, XylHCl) up to about 0.1 GPa only, but still higher pressure destabilizes this structure. Above 0.1 GPa, XylHCl preferentially crystallizes as solvates with CH2Cl2, CHCl3, or (CH3)2CHOH depending on the solvent used. However, when XylHCl·H2O is dissolved in any of these solvents, the high-pressure crystallizations yield the hydrate XylHCl·H2O only. The single crystals of the CH2Cl2, CHCl3, and (CH3)2CHOH solvates could be grown in situ in a diamond anvil cell, which allowed their structure determination from the …
A case of bowel schistosomiasis not adhering to endoscopic findings
2005
Schistosomiasis is a chronic worm infection caused by a species of trematodes, the Schistosomes. We may distinguish a urinary form from Schistosomes haematobium and an intestinal-hepatosplenic form mainly from Schistosomes mansoni characterized by nausea, meteorism, abdominal pain, bloody diarrhea, rectal tenesmus, and hepatosplenomegaly. These infections represent a major health issue in Africa, Asia, and South America, but recently S mansoni has increased its prevalence in other continents, such as Europe countries and North America, due to international travelers and immigrants, with several diagnostic and prevention problems. We report a case of a 24-year-old patient without HIV infecti…
Treatment of Ulcerative Colitis with Olsalazine and Sulphasalazine: Efficacy and Side-Effects
1988
The effects of olsalazine were studied mainly in patients with ulcerative colitis who were intolerant to sulphasalazine, and for relapse prevention. A crossover design with sulphasalazine, 3 g/day, and olsalazine, 1.5 g/day, was applied to compare the side-effects of each drug and to evaluate their therapeutic efficacy. A total of 41 patients with mild or moderately severe left-sided colitis or proctitis were assigned to a randomized treatment schedule. Olsalazine and sulphasalazine were similar in their therapeutic efficacy. Twelve patients complained of adverse effects while on sulphasalazine and 4 patients during olsalazine treatment (p less than 0.05). It is concluded that olsalazine is…
Non-chemotherapy drug-induced agranulocytosis in a tertiary hospital
2015
Drug-induced agranulocytosis is a rare haematological disorder considered as severe adverse drug reaction. Due to its low incidence, the number of studies are low and the variability of clinical features and presentation in hospitalized patients is rarely described. Awe performed an observational, transversal and retrospective study in the haematology and toxicology unit in a tertiary hospital located in Spain (Valencia) (1996–2010) in order to assess its incidence, the drugs involved, the management and outcomes of drug-induced agranulocytosis. Twenty-one cases of agranulocytosis were retrieved. All of them presented severe and symptomatic agranulocytosis (fever and infection). The most c…
Antiinflammatory treatment and intestinal alpha 1-antitrypsin clearance in active Crohn's disease.
1985
Intestinal alpha 1-antitrypsin clearance was quantified in 17 patients with clinically active Crohn's disease before and after a six-week period of treatment with sulfasalazine and methylprednisolone. Before the study, alpha 1-antitrypsin clearance and, hence, enteric protein loss was elevated as being above control values in 16 patients. After therapy, clearance values decreased in 11 and were normalized in five patients. Serum albumin level was normalized in 11 of 12 patients who had hypoalbuminemia before the study. Clinical condition was improved in all but 1 patient after treatment. There was no close correlation between alpha 1-antitrypsin clearance and disease activity index. These r…
Job absenteeism and arterial hypertension: results of a hypertension control program.
1992
This study reports the findings of one of the stages of a programme for the detection and control of arterial hypertension, started in I980 in an automobile company with a workforce of 9,782. In the initial screening, 522 hypertensive males were found using epidemiological criteria and 206 of these fulfilled the criteria of definite hypertension. The objective of this study consisted of evaluating, 9 years after the start of the program, the indirect cost in terms of the reduction in the morbidity indicator-temporary work incapacity (TWI). Analysis is based on a comparison of the prevalence of hypertension in the population when the program was begun (6%) and in 1989 (9.8%). It can be obser…