Search results for "Propanolamines"
showing 10 items of 23 documents
Quantitation of talinolol in rat plasma by LC-MS-MS.
2010
The aim of this study was to develop and validate an assay based on liquid chromatography-tandem mass spectrometry to quantitate talinolol in rat plasma. After a simple protein precipitation step, separation was performed by reversed-phase liquid chromatography using gradient elution with acetonitrile-water-formic acid. Electrospray ionization in the positive ion mode with multiple reaction monitoring was used to analyze talinolol employing propranolol as internal standard. The calibration curve for talinolol was linear over the concentration range 1-250 ng/mL with a correlation coefficient0.995. The method was sensitive (limit of quantitation, 1 ng/mL) and had acceptable accuracy (85-115% …
Bidirectional membrane transport: Simulations of transport inhibition in uptake studies explain data obtained with flavonoids
2006
The purpose of the simulations was to obtain an estimate of concentration-dependent uptake curves when two counteracting transporters are present. On the basis of this experimental data obtained with a pair of ovarian carcinoma cell lines, one of which was not expressing the exsorptive transporter P-glycoprotein and one of which was an MDR1-transfected, P-glycoprotein expressing variant, the kinetics of cellular uptake of the radiolabel (3)H-talinolol were calculated and the inhibitory constants at P-gp were determined for different flavonoids. With respect to the inhibition of P-gp function, among others, naringenin and isoquercitrin were identified as inhibitors, yet estimation of the inh…
Bile acid amidoalcohols: simple organogelators.
2003
Simple bile acid amide synthesis of lithocholic and deoxycholic acids with 2-aminoethanol and 3-aminopropanol are reported. The structural properties of these amides were examined by NMR spectroscopic, ESI-TOF mass spectral, and X-ray crystallographic methods. The gelation properties of these amides in common organic solvents and in three different water solutions were also investigated using Tyndall effect, SEM, TEM, and optical microscopy. 2-Hydroxyethylamides were found to be effective gelators in chlorinated organic solvents and 3-hydroxypropylamides in aromatic solvents. Both derivatives thicken neutral and acidic water solutions.
Systematic review with meta-analysis: the haemodynamic effects of carvedilol compared with propranolol for portal hypertension in cirrhosis
2013
Summary Background Propranolol is recommended for prophylaxis of variceal bleeding in cirrhosis. Carvedilol is a nonselective beta-blocker with a mild anti-alfa-1-adrenergic activity. Several studies have compared carvedilol and propranolol, yielding inconsistent results. Aim To perform a systematic review and meta-analysis of the randomised clinical trials comparing carvedilol with propranolol for hepatic vein pressure gradient reduction. Methods Studies were searched on the MEDLINE, EMBASE and Cochrane library databases up to November 2013. The weighted mean difference in percent hepatic vein pressure gradient reduction and the relative risk of failure to achieve a hemodynamic response (r…
Beta-adrenoceptor density and subtype distribution in cerebellum and hippocampus from patients with Alzheimer's disease
1993
beta-Adrenoceptor density and beta 1- and beta 2-subtype distribution were examined in hippocampi and cerebella from patients with Alzheimer's disease (AD/SDAT). Tissues from age-, sex and post-mortem delay matched non-demented patients served as controls. The total beta-adrenoceptor density as evaluated in saturation experiments with the hydrophilic radioligand [3H]CGP 12177 was higher in hippocampal (36-39 fmol/mg protein) than cerebellar tissues (20-21 fmol/mg), however, no differences were found in either brain region between AD/SDAT patients and controls. Subtype distribution using the highly selective beta 1-adrenoceptor antagonist CGP 20712A revealed a slightly higher proportion of b…
Pretreatment with potent P-glycoprotein ligands may increase intestinal secretion in rats.
2001
The expression of P-glycoprotein is induced in cell cultures upon exposure to various inducers. Therefore, the aim of the present study was to evaluate the in-vivo relevance of this observation, i.e. the influence of chronic pretreatments with selected drugs -- all of which are ligands to P-glycoprotein (P-gp) as demonstrated in radioligand binding studies and all of which have some or a considerable effect on P-gp expression in Caco-2 cells -- on the effective intestinal permeabilities of the model compound talinolol in rats employing in-situ single-pass intestinal perfusion of three different gut segments. Talinolol was selected, because it shows high selectivity for one of the exsorptive…
Short-term adaptation of conditioned fear responses through endocannabinoid signaling in the central amygdala
2010
International audience; Both, the cannabinoid receptor type 1 (CB1) and the central nucleus of the amygdala (CeA) are known to play crucial roles in the processing of fear and anxiety, whereby they appear to be especially involved in the control of fear states. However, in contrast to many other brain regions including the cortical subregions of the amygdala, the existence of CB1 in the CeA remains enigmatic. Here we show that CB1 is expressed in the CeA of mice and that CB1 in the CeA mediates short-term synaptic plasticity, namely depolarization-induced suppression of excitation (DSE) and inhibition (DSI). Moreover, the CB1 antagonist AM251 increased both excitatory and inhibitory postsyn…
Origin and correction of the deviations in retention times at increasing flow rate with Chromolith columns.
2010
Chromoliths can be used at flow rates beyond those feasible for conventional microparticulate packed columns. Ideally, the plots of the retention time versus the inverse of delivered flow rate should exhibit y-intercept of zero. However, significant positive deviations correlating with the solute polarity were observed for several compounds chromatographed with a Chromolith column, owing to the increased system pressure. Consequently, the dead time marker exhibits a smaller deviation, making the retention factors depend on the flow rate. Chromoliths are made of a silica-based monolith encapsulated within a PEEK tube, and should suffer larger stress with pressure than stainless steel columns…
Modulation of drug transport by selected flavonoids: Involvement of P-gp and OCT?
2004
Flavonoids, as a common component of daily nutrition, are a possible source of interference with absorption processes, due to modulation of transporting proteins. In this study, the influence of selected flavonoids (quercetin, isoquercitrin, spiraeoside, rutin, kaempferol, naringenin, naringin, and kaempferol) on the transport of the P-gp substrate [3H]talinolol across Caco-2 cell monolayers was investigated. To elucidate the mechanism behind the interaction observed in this system the potency of the flavonoids to replace [3H]talinolol from its P-gp binding site as well as their activity to inhibit OCT2-mediated [14C]TEA uptake into LLC-PK(1) cells were measured, as P-gp and OCT have been s…
Different Dissolution Media Lead to Different Crystal Structures of Talinolol with Impact on Its Dissolution and Solubility
2003
During the performance of dissolution tests with immediate and controlled-release talinolol tablets it was detected that the type of the buffer used as dissolution medium had a strong influence on the solubility and the dissolution behavior of the drug. It was proven that talinolol appeared in different crystal structures with strongly differing solubilities when pure water, acetate, or phosphate buffers were employed as dissolution media. The resulting crystal structures were characterized by means of light microscopy, differential scanning calorimetry, and X-ray powder diffraction. All methods were adjuvant to detect changes in talinolol crystal structures. The different solubility and di…