Search results for "INDOMETHACIN"
showing 10 items of 85 documents
Influence of Polymer Molecular Weight on Drug–polymer Solubility: A Comparison between Experimentally Determined Solubility in PVP and Prediction Der…
2015
ABSTRACT: In this study, the influence of polymer molecular weight on drug–polymer solubility was investigated using binary systems containing indomethacin (IMC) and polyvinylpyrrolidone (PVP) of different molecular weights. The experimental solubility in PVP, measured using a differential scanning calorimetry annealing method, was compared with the solubility calculated from the solubility of the drug in the liquid analogue N-vinylpyrrolidone (NVP). The experimental solubility of IMC in the low-molecular-weight PVP K12 was not significantly different from that in the higher molecular weight PVPs (K25, K30, and K90). The calculated solubilities derived from the solubility in NVP (0.31–0.32 …
Anti-inflammatory activity in mice of extracts from Mediterranean marine invertebrates.
1998
The effects of dichloromethane and methanol extracts from the marine invertebrates Leptogorgia ceratophyta, Holothuria tubulosa, Coscinasterias tenuispina and Phallusia fumigata on carrageenan-induced paw oedema in mice were investigated. The dichloromethane extract of Coscinasterias tenuispina and the methanol extract of Holothuria tubulosa administered p.o. at 50, 100 and 150 mg/kg, inhibited oedema in a dose-dependent manner 3 h after administration of carrageenan. Both extracts partially decreased elastase activity and PGE2 levels measured in homogenates from inflamed paws, without affecting the levels of this prostanoid present in stomach homogenates. As observed with the selective inh…
Comparison of the contractile effects of endothelin-1 and sarafotoxin S6b in goat isolated cerebral arteries
1992
1. The effects of endothelium-derived endothelin-1 and snake venom-derived sarafotoxin S6b, peptides with striking structural and functional similarities, were examined and compared in isolated middle cerebral arteries of goats. 2. Endothelin-1 and sarafotoxin S6b contracted cerebral arteries in a concentration-dependent manner. The potency of endothelin-1 (EC50 = 4.9 (3.9-6.2) x 10(-10) M) was about ten times higher than that of sarafotoxin S6b (EC50 = 5.5 (4.4-6.9) x 10(-9) M). The tension returned to basal values after repeated washings and contraction with endothelin-1 could be reproduced. Endothelin-1 and sarafotoxin S6b induced further contraction in arteries precontracted with prosta…
Beta-adrenoceptor-mediated facilitation of endogenous noradrenaline release from rat isolated trachea.
1994
Overflow of endogenous noradrenaline from rat isolated trachea was evoked by electrical field stimulation (3 Hz, 540 pulses) in the presence of yohimbine, desipramine and tyrosine. Isoprenaline 100 nmol/l increased the evoked overflow of noradrenaline by about 65%. This effect was antagonized by propranolol (100 nmol/l) and the beta 2-selective adrenoceptor antagonist ICI 118,551 (100 nmol/l), but not by the beta 1-selective adrenoceptor antagonist CGP 20712 A (100 nmol/l). The beta 2-selective adrenoceptor agonist formoterol (1-100 nmol/l) also facilitated the evoked overflow of noradrenaline, but maximally by only about 25% at 10 nmol/l, i.e. formoterol behaved as a partial agonist at the…
Intermittent ethanol exposure induces inflammatory brain damage and causes long-term behavioural alterations in adolescent rats
2007
Adolescent brain development seems to be important for the maturation of brain structures and behaviour. Intermittent binge ethanol drinking is common among adolescents, and this type of drinking can induce brain damage. Because we have demonstrated that chronic ethanol treatment induces inflammatory processes in the brain, we investigate whether intermittent ethanol intoxication enhances cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) in adolescent rats, and whether these mediators induce brain damage and cause permanent cognitive dysfunctions. Adolescent rats were exposed to ethanol (3.0 g/kg) for two consecutive days at 48-h intervals over 14 days. Levels of COX-2, iN…
Rhein stimulates active chloride secretion in the short-circuited rat colonic mucosa.
1988
In a short-circuited mucosa-submucosa preparation of the rat descending colon with preserved Meissner's plexus mounted as an everted sac rhein transiently increased the potential difference and short-circuit current (Isc) when administered serosally and mucosally, but serosal application was more effective. Maximal effects were obtained at rhein concentrations of 1.6 X 10(-4) and 3 X 10(-4) mol/l. Net chloride absorption was decreased. Indomethacin (5 X 10(-6) mol/l) did not inhibit the increase of Isc, but omission of calcium from the serosal side as well as tetrodoxin (2 X 10(-7) mol/l) decreased it by 50 and 60%. Mechanical removal of Meissner's plexus partly blocked the effect of rhein,…
Effect of the stable prostacyclin analogue iloprost on water and electrolyte transfer of the rat ileum and colon in vivo.
1988
The effect of iloprost on water and ion transfer was measured simultaneously in tied-off loops of the rat ileum and colon in vivo. (1) In the ileal loops iloprost had no effect on water and ion transfer neither by intraluminal, nor intraaortal or intravenous application. (2) In the colonic loops only intraaortal bolus application of the high dose of 500 micrograms iloprost significantly decreased net water, sodium and chloride absorption, but did not induce net secretion. (3) Inhibition of endogenous prostaglandin synthesis by indomethacin did not change net water and electrolyte transfer in the ileum and colon. (4) Under this pretreatment i.v.-application of 100 micrograms iloprost, ineffe…
Nonsteroidal Anti-Inflammatory Drugs and Ectodomain Shedding of the Amyloid Precursor Protein
2008
<i>Background:</i> Epidemiological studies have suggested that long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with a reduced incidence of Alzheimer’s disease (AD). Several mechanisms have been proposed to explain these findings including increased shedding of the soluble ectodomain of the amyloid precursor protein (sAPP), which functions as a neurotrophic and neuroprotective factor in vitroand in vivo. <i>Objective:</i> To clarify whether NSAIDs consistently stimulate sAPP secretion. <i>Methods:</i> 293-EBNA cells with stable overexpression of an APP-alkaline phosphatase fusion protein (APP-AP), SH-SY5Y and PC12 cells or prim…
Pentobarbital-sensitive EDHF comediates ACh-induced arteriolar dilation in the hamster microcirculation
1999
It is unclear to what extent the endothelium-derived hyperpolarizing factor (EDHF) contributes to the control of microcirculatory blood flow in vivo. We analyzed, by intravital microscopy in hamster muscles, the potential role of EDHF along the vascular tree under stimulated (ACh) or basal conditions. Experiments were performed in conscious as well as anesthetized (pentobarbital, urethan) animals. Additionally, cellular effects of the potential EDHF were studied in isolated small arteries. In pentobarbital-anesthetized animals, treatment with N ω-nitro-l-arginine (l-NNA; 30 μmol/l) and indomethacin (3 μmol/l) reduced the dilation in response to 10 μmol/l ACh from 60 ± 6 to 20 ± 4%. This ni…
Epithelium-derived inhibition of [3H]acetylcholine release from the isolated guinea-pig trachea
1990
To investigate presynaptic, regulatory mechanisms on parasympathetic nerve fibres innervating the airways, the release of newly-synthesized [3H]acetylcholine from the isolated trachea was studied. Reverse phase HPLC followed by liquid scintillation spectrometry was used to separate and quantify the radioactive compounds choline, phosphorylcholine and acetylcholine in the incubation medium and the tissue. During the incubation of the tracheae with [3H]choline a significant synthesis of [3H]acetylcholine (35,000 dpm/preparation) and [3H]phosphorylcholine (500,000 dpm/preparation) occurred. In epithelium-deficient tracheae the formation of [3H]phosphorylcholine was enhanced, whereas the conten…