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Showing papers in "European Journal of Pharmacology in 2002"


Journal ArticleDOI
TL;DR: Aripiprazole is the first dopamine-serotonin system stabilizer, according to a study demonstrating potent, partial agonism at 5-HT(1A) receptors in a guanosine-5'-O-(3-[( 35)S]thio)-triphosphate ([(35)S)GTP gamma S)-binding assay.

467 citations


Journal ArticleDOI
TL;DR: Changes in glutamate receptor subtypes, in second-messenger systems and in protein kinases that may account for the alterations in synaptic plasticity are discussed, which may allow treatment or prevention of this diabetic complication in the future.

466 citations


Journal ArticleDOI
TL;DR: The theoretical possibility that GHS analogues could become candidate drugs for treatment of pathophysiological conditions in internal medicine totally unrelated to disorders of GH secretion is confronted, particularly, GHS receptor agonists or antagonists acting on appetite could represent new drug intervention in eating disorders.

399 citations


Journal ArticleDOI
TL;DR: There is no common agreement about the extent to which salicylate contributes to aspirin's anti-inflammatory properties, as well as there is still no final conclusion reached about the mechanisms of action of sodium salicYLate.

317 citations


Journal ArticleDOI
TL;DR: Recent progress in the understanding of the physiological activity of neutrophil elastase and its role in acute lung injury is reviewed to support the involvement of this enzyme in the pathophysiology of acute lungs injury.

297 citations


Journal ArticleDOI
TL;DR: It is suggested that pteropodine and isopteropodines act as positive modulators of muscarinic M(1) and 5-HT(2) receptors.

295 citations


Journal ArticleDOI
TL;DR: This review will describe the current literature on the biochemistry of ACRP30 and its physiological functions and discuss issues that are relevant to the directions of future research.

277 citations


Journal ArticleDOI
TL;DR: The hypothesis that superoxide anions play an important role in gentamicin-mediated nephropathy is confirmed and the possible clinical use of low molecular weight synthetic superoxide dismutase mimetics in those conditions that are associated with over production of superoxide is supported.

265 citations


Journal ArticleDOI
TL;DR: The results implicate ATP as a primary signalling molecule in glial cells and indicate specific roles for P2Y and P2X purinoceptors inglial cell pathology.

239 citations


Journal ArticleDOI
TL;DR: Over a 1-year period, obese patients taking orlistat in combination with a hypocaloric diet show a reduction of 2-5 kg over the weight decrease with placebo, and when continued for a second year in conjunction with a weight maintenance diet, orlistats reduces weight regain compared to placebo-treated patients.

234 citations


Journal ArticleDOI
TL;DR: The inhibition of bone resorption obtained specifically with S12911-2 is related to an inhibition of the differentiation and resorbing activity of the osteoclasts.

Journal ArticleDOI
TL;DR: The ratio of total plasma drug concentration to HERG IC(50) value was indicative of the degree of QT prolongation observed and target receptor affinity and expected clinical plasma levels are important parameters to consider for the interpretation of HERG channel data.

Journal ArticleDOI
TL;DR: Results clearly indicate that T-226296 is a novel, orally active and selective MCH receptor antagonist that will be promising for further exploring the physiology and pathophysiology of MCH-SLC-1 signaling.

Journal ArticleDOI
TL;DR: Acute neutrophil stimulation could facilitate antibacterial effects of azithromycin, while delayed, potentially anti-inflammatory activity may curtail deleterious inflammation.

Journal ArticleDOI
TL;DR: Data obtained both in vitro and in vivo suggest that wogonin and quercetin exert inhibitory activity on lipopolysaccharide-induced NO production through suppression of iNOS expression.

Journal ArticleDOI
TL;DR: Supporting a role for the CRF system in the regulation of energy balance are findings demonstrating alterations in this system in obese and food-deprived animals that concur to facilitate energy deposition.

Journal ArticleDOI
TL;DR: It is demonstrated that anandamide and its analog, O-1812, are anticonvulsant in a whole animal model and further implicate the cannabinoid CB(1) receptor as a major endogenous site of seizure modulation.

Journal ArticleDOI
TL;DR: β 3 -adrenoceptor agonists have a more rapid insulin-sensitising than anti-obesity effect, possibly because stimulation of lipid oxidation rapidly lowers intracellular long-chain fatty acyl CoA and diacylglycerol levels, which may deactivate those protein kinase C isoenzymes that inhibit insulin signalling.

Journal ArticleDOI
TL;DR: Data suggest that forebrain regions innervated by these two distinct noradrenergic pathways exert opposing influences on the behavioral response to reboxetine in the rat forced swim test.

Journal ArticleDOI
TL;DR: The results suggest that both caffeic acid and rosmarinic acid may produce antidepressive-like activity via some mechanism(s) other than the inhibition of monoamine transporters and monoamine oxidase.

Journal ArticleDOI
TL;DR: Evidence concerning the role of the renin-angiotensin system in learning and memory is contradictory, although more studies support the proposal that ang Elliotensin reduces cognitive function.

Journal ArticleDOI
TL;DR: The effects of the kappa-opioid receptor agonist, TRK-820, (-)-17-(cyclopropylmethyl)-3, 14beta-dihydroxy-4, 5alpha-epoxy-6beta-[N-methyl-trans-3-(3-furyl) acrylamido] morphinan hydrochloride, on the itch sensation were compared with those of histamine H1 receptor antagonists, using the mouse pruritogen-induced scratching model as discussed by the authors.

Journal ArticleDOI
TL;DR: The data of this study indicate that a planar structure is necessary for high inhibitory activity towards xanthine oxidase, and the contribution of a hydroxyl conjugate turns out to be a constant factor when the natural logarithm of IC(50) values is taken.

Journal ArticleDOI
TL;DR: It is shown that intrathecal omega-conotoxins are effective in attenuating tactile allodynia in the rat without significantly affecting acute nociceptive responses.

Journal ArticleDOI
TL;DR: Zaleplon potentiated GABA-evoked Cl(-) currents in Xenopus oocytes expressing human GABA(A) receptor subunits with a potency that was higher at alpha1beta2gamma2 receptors than at alpha2- or alpha3-containing receptors.

Journal ArticleDOI
TL;DR: Findings show that pirfenidone inhibits the production of the proinflammatory cytokine selectively at the translational level, and that this inhibitory effect is selective, translational, and not for total protein synthesis, suggesting this drug may have a clinical effect on inflammation and fibrosis with very low toxicity.

Journal ArticleDOI
TL;DR: The potential involvement of extracellular ATP and P2X7 receptors as regulators of interleukin-1-mediated neuropathologies and thus as a mediator of cell death following pathological insults is discussed.

Journal ArticleDOI
TL;DR: EAhy926 endothelial cells are an adequate tool to substantiate and characterize inflammatory impacts of PPAR activators and had the greatest potency to reduce cytokine-induced monocyte chemotactic protein-1 (MCP-1) secretion.

Journal ArticleDOI
Bertil Waldeck1
TL;DR: Inhaled beta(2)-adrenoceptor agonists are by far the most effective and safe bronchodilators currently available as discussed by the authors, and they have not been surpassed by any other bronchodorizing principle.

Journal ArticleDOI
TL;DR: The results suggest that relief from cancer pain by morphine inhibits tumor growth and metastasis.