Abstract：
:Nonsteroidal anti-inflammatory drugs (NSAID) inhibit cyclooxygenase activity and cause gastrointestinal damage in part by promoting leukocyte accumulation in the mucosa. Our aim was to evaluate the effects of selective blockade of the isoenzymes cyclooxygenase-1 and cyclooxygenase-2 on leukocyte adhesion in vivo. Leukocyte/endothelial cell interactions were examined in rat mesenteric venules before and after treatment with indomethacin, SC-560 (5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethylpyrazole, cyclooxygenase-1 inhibitor), DFP (5,5-dimethyl-3-(2-propoxy)-4-(4-methanesulfonyl)-2(5H)-furanone, cyclooxygenase-2 inhibitor), or SC-560 plus DFP (20 mg/kg, i.v. each). Indomethacin increased leukocyte-rolling flux, reduced rolling velocity and elicited significant leukocyte adhesion. Neither SC-560 nor DFP induced these effects although their co-administration reproduced the indomethacin response. Indomethacin and SC-560, but not DFP, abolished cyclooxygenase-1 activity in blood. Plasma from indomethacin- or DFP-, but not from SC-560-treated rats abolished cyclooxygenase-2 activity in activated A549 cells. Specific blockade of cyclooxygenase-1 or cyclooxygenase-2 does not induce any inflammatory event in the rat mesentery and the inflammatory response observed with non-selective NSAIDs seems to be due to the inhibition of both isoenzymes.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Calatayud S,Mitchell JA,Perretti M,Giuliano F,Warner TDdoi
10.1016/s0014-2999(02)01342-0keywords:
subject
Has Abstractpub_date
2002-04-05 00:00:00pages
71-7issue
1eissn
0014-2999issn
1879-0712pii
S0014299902013420journal_volume
440pub_type
杂志文章abstract：:Peripheral type benzodiazepine receptors are differentially modified by arachidonate, diethylpyrocarbonate and thiol reagents, as evidenced by the finding that binding of a proposed agonist ([3H]R05-4864) and a proposed antagonist ([3H]PK 11195) to rat kidney mitochondrial membranes can be modified separately. (1) Ara...
journal_title：European journal of pharmacology
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更新日期：1991-12-12 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1991-10-29 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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更新日期：2003-11-07 00:00:00
