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Activity of nimesulide on constitutive and inducible cyclooxygenases.
Prostaglandins are pro-inflammatory but are gastroprotective. The gastric mucosa synthesizes prostaglandins mainly via constitutive cyclooxygenase (COX-1), whereas leucocytes have inducible enzymeExpand
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Early Responses to Dynamic Strain Change and Prostaglandins in Bone‐Derived Cells in Culture
Mechanical loading of bone explants stimulates prostaglandin E2 (PGE2) and prostacyclin (PGI2) release and increases glucose 6‐phosphate dehydrogenase (G6PD) activity. This response is blocked byExpand
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Prostate-derived Sterile 20-like Kinases (PSKs/TAOKs) Phosphorylate Tau Protein and Are Activated in Tangle-bearing Neurons in Alzheimer Disease*
Background: Neurofibrillary tangles comprising abnormally phosphorylated tau are hallmarks for Alzheimer disease. Results: Prostate-derived sterile 20-like kinases (PSKs) phosphorylate tau on moreExpand
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Pharmacokinetics of dexloxiglumide after administration of single and repeat oral escalating doses in healthy young males.
OBJECTIVE To assess the pharmacokinetics, safety and tolerability of dexloxiglumide, a new CCK1 receptor antagonist currently under development for the treatment of the constipation-predominantExpand
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Loading‐related increases in prostaglandin production in cores of adult canine cancellous bone in vitro: A role for prostacyclin in adaptive bone remodeling?
Cyclic mechanical loading sufficient to engender strains of physiologic magnitude applied to recently excised canine cancellous bone cores in vitro increased the release of prostaglandin E (PGE) andExpand
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Comparison of indomethacin and nimesulide, a selective cyclooxygenase-2 inhibitor, on key pathophysiologic steps in the pathogenesis of nonsteroidal anti-inflammatory drug enteropathy in the rat.
BACKGROUND The predicted gastrointestinal tolerability of specific cyclooxygenase-2 inhibitors could be due to either a lack of 'topical' irritation and/or lack of effect on cyclooxygenase-1. Expand
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Pharmacological characterization of cholecystokinin receptors mediating contraction of human gallbladder and ascending colon
Cholecystokinin (CCK) produces contractions of gallbladder and colon in a number of different species. Although the effects of CCK on the human gallbladder are relatively well documented, the CCKExpand
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The biological activities of phthalate esters on rat gastric muscle.
Monoethylhexyl phthalate, at concentrations that can occur in blood stored in plastic bags (0.1-0.5 mg/ml), reduced contractions of rat isolated gastric fundus to PGE2 and acetylcholine; the diethylExpand
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Prostate-derived Sterile 20-like Kinase 2 (PSK2) Regulates Apoptotic Morphology via C-Jun N-terminal Kinase and Rho Kinase-1*
We have reported previously that human prostate-derived sterile 20-like kinase (PSK) 1 alters actin cytoskeletal organization and binds to microtubules, regulating their organization and stability.Expand
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Pharmacological evidence for putative CCK1 receptor heterogeneity in human colon smooth muscle
The pharmacology of the cholecystokinin CCK1 receptors endogenously expressed in human gallbladder and human ascending colon smooth muscle tissue was compared using radioligand binding assays.Expand
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