Search results for "BUP"
showing 10 items of 168 documents
Patterns of flower development in Apiaceae–Apioideae
2016
Abstract Apiaceae is a large family characterized by uniform flowers. However, early ontogenetic studies revealed unexpected diversity in flower development. In the present paper, we investigate eight species representing six tribes of subfamily Apioideae to address diversity in developmental patterns. One focus is on the developmental divergence of sex morphs in andromonoecious species. Scanning electron microscopic studies were conducted on six herbaceous species: Chaerophyllum bulbosum , Daucus carota , Dorema aucheri , Ferula hezarlalehzarica , Orlaya grandiflora , Pastinaca sativa , and two woody species, i.e., Bupleurum fruticosum and Seseli ghafoorianum . Our results confirm the exis…
Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin.
2017
A single high-affinity fatty acid binding site in the important human transport protein serum albumin (HSA) is identified and characterized using an NBD (7-nitrobenz-2-oxa-1,3-diazol-4-yl)-C12 fatty acid. This ligand exhibits a 1:1 binding stoichiometry in its HSA complex with high site-specificity. The complex dissociation constant is determined by titration experiments as well as radioactive equilibrium dialysis. Competition experiments with the known HSA-binding drugs warfarin and ibuprofen confirm the new binding site to be different from Sudlow-sites I and II. These binding studies are extended to other albumin binders and fatty acid derivatives. Furthermore an X-ray crystal structure …
Safety and efficacy of buparlisib (BKM120) and chemotherapy in advanced, squamous non-small cell lung cancer (sqNSCLC): Results from the phase Ib/II …
2016
e20522Background: Phosphatidylinositol 3-kinase (PI3K) pathway activation may contribute to primary and secondary resistance to platinum (Pt)-based chemotherapy (CT) in sqNSCLC. The pan-PI3K inhibi...
Effects of ibuprofen and carbamazepine on the ion transport system and fatty acid metabolism of temperature conditioned juveniles of Solea senegalens…
2018
The increasing presence of pharmaceuticals in aquatic environments in the last decades, derived from human and veterinary use, has become an important environmental problem. Previous studies have shown that ibuprofen (IB) and carbamazepine (CBZ) modify physiological and biochemical processes in Senegalese sole (Solea senegalensis) in a temperature-dependent manner. In other vertebrates, there is evidence that both of these pharmaceuticals interfere with the ‘arachidonic acid (AA) cascade’, which is responsible for the biosynthesis of numerous enzymes that are involved in the osmoregulatory process. The present work aims to study the temperature-dependent effects of these two pharmaceuticals…
Adolescent and adult mice display differential sensitivity to the effects of bupropion on the acquisition of a water maze task.
2017
Abstract Background Adolescence is characterized by major neurobiological changes, and the effects of some psychoactive drugs seem to differ between adolescents and adults. Bupropion, an antidepressant that is also used to treat nicotine addiction, induces behavioral actions in both adolescent and adult rodents. However, the effects of this drug on spatial ability have not been compared in animals at different stages of their development. The present study was conducted to assess the effects of bupropion on spatial learning and memory in adolescent and adult mice. Methods Adolescent (post-natal day: PND35-36) and adult (PND >65) NMRI mice received bupropion (10, 20 and 40 mg/kg) or saline d…
A Comprehensive Spectroscopic Analysis of the Ibuprofen Binding with Human Serum Albumin, Part I
2020
Human serum albumin (HSA) plays a fundamental role in the human body. It takes part in the transport of exogenic and endogenic substances, especially drugs. Ibuprofen (IBU) is one of the most commonly used non-steroidal anti-inflammatory drugs, used for pain relief, fever relief, and for anti-inflammatory purposes. The binding of ligands with HSA is a significant factor which determines the toxicity and the therapeutic dosages of these substances. The aim of this study was to compare the degree of ibuprofen binding with human serum albumin at various temperatures and protein solution pH values. In order to evaluate conformational changes in HSA caused by interaction with ibuprofen, spectrop…
Efectos de la hiperamonemia y la encefalopatía hepática sobre la conectividad neuronal en cerebro de pacientes cirróticos y modelos animales. Implica…
2018
La encefalopatía hepática (HE) es un complejo síndrome neuropsiquiátrico producido por la alteración en la función del sistema nervioso central asociada a la cirrosis hepática. Entre un 33-55% de los pacientes cirróticos sin síntomas clínicos evidentes de EH padecen encefalopatía hepática mínima (EHM) con deterioro cognitivo leve que empeora su calidad y esperanza de vida. Los pacientes cirróticos con EHM presentan alteraciones en la generación del potencial MMN (Mismatch Negativity), concretamente una disminución del área bajo la curva del potencial, que se correlaciona con los déficits de atención. En esta tesis hemos demostrado que las ratas con hiperamonemia crónica reproducen las alter…
Buprenorfina-naloxona en el tratamiento de la dependencia a opiáceos
2007
En los últimos diez años la buprenorfina ha aumentado su disponibilidad en Europa como alternativa a la metadona en el tratamiento de la dependencia a opiáceos. La buprenorfina es un opiáceo sintético con actividad agonista parcial utilizado en el tratamiento de sustitución de la dependencia a opiáceos. Diversos estudios han demostrado que posee una eficacia superior a placebo y similar a metadona.Con el fin de disminuir el uso inadecuado de la buprenorfina por vía intravenosa, en octubre de 2002 se aprobó en Estados Unidos la combinación sublingual de buprenorfina con una pequeña dosis del antagonista opiáceo naloxona. Sin embargo, no es hasta octubre de 2006 cuando la Comisión Europea apr…
Effect of epidural anesthesia on colorectal anastomosis: a tonometric assessment.
1997
PURPOSE: Epidural anesthesia is believed to benefit colorectal anastomotic blood flow because of the sympathetic blockade it produces. Our purpose is to measure with tonometry the effect of epidural anesthesia on colorectal anastomotic oxygenation. PATIENTS AND METHODS: Fifteen patients operated on for rectal cancer (radical anterior resection) were monitored postoperatively using tonometers placed in the stomach (celiac trunk), transverse colon (superior mesenteric artery), and the anastomotic area during the operation. An epidural catheter was placed at L1-2, and on the first postoperative day, 8 ml of bupivacaine (0.25 percent) was administered. The anesthetic effect extended up to T-4. …
A novel technique for intraduodenal administration of drug suspensions/solutions with concurrent pH monitoring applied to ibuprofen formulations
2019
Characterization of dissolution of solid suspended drug particles in vivo is important for developing biopredictive in vitro tests. Therefore, methods to gain deeper insights into particle dissolution in vivo are needed. The soft Bioperm intubation method, a well established tool for investigation of permeability, absorption, metabolism, and drug interactions at predefined locations in the gastroinstinal tract, was modified. The novel intubation method involved pump-controlled infusion of pharmaceutical suspensions as well as simultaneous pH monitoring. This technique was used in a proof of concept study in healthy humans. Plasma sampling and non-compartmental analysis allowed comparison of…