{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,31]],"date-time":"2026-08-31T09:41:30Z","timestamp":1788169290158,"version":"build-2803163510"},"reference-count":35,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2009,1,29]],"date-time":"2009-01-29T00:00:00Z","timestamp":1233187200000},"content-version":"vor","delay-in-days":3591,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[1999,4]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>In this study we describe experiments to establish <jats:italic>ex vivo<\/jats:italic> the selectivity of non\u2010steroidal anti\u2010inflammatory drugs (NSAIDs) given <jats:italic>in vivo<\/jats:italic>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Anaesthetised (Inactin, 120\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup>) male Wistar rats (220\u2013250\u2003g) received an i.v. dose of one of the following compounds (dose mg\u2003kg<jats:sup>\u22121<\/jats:sup>): aspirin (20), diclofenac (3), L\u2010745,337 (30), nimesulide (15), salicylate (20), sulindac (10). Blood samples were taken before and up to 6\u2003h after dosing and the plasma obtained from it was tested for its ability to inhibit prostanoid formation in IL\u20101\u03b2\u2010treated A549 cells (COX\u20102 system) and human washed platelets (COX\u20101 system). For control the same compounds were also added directly to the assay systems.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>All drugs, except sodium salicylate, inhibited COX\u20101 and COX\u20102 when added directly to the test systems. Plasma from aspirin\u2010treated rats was without effect on either COX\u20101 or COX\u20102, consistent with the rapid <jats:italic>in vivo<\/jats:italic> metabolism to salicylate. Conversely, plasma from sulindac\u2010treated rats inhibited COX\u20101 and COX\u20102 with potencies according with <jats:italic>in vivo<\/jats:italic> metabolism to sulindac sulphide. Diclofenac was COX\u20101\/2 non\u2010selective when tested <jats:italic>in vitro<\/jats:italic>, but a slightly preferential inhibitor of COX\u20102 when tested <jats:italic>ex vivo<\/jats:italic>. Nimesulide was confirmed as preferential inhibitor of COX\u20102 both <jats:italic>in vitro<\/jats:italic> and <jats:italic>ex vivo<\/jats:italic>. L\u2010745,337 was a selective COX\u20102 inhibitor when tested <jats:italic>in vitro<\/jats:italic> or <jats:italic>ex vivo<\/jats:italic>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>In conclusion, our experiments show clearly (a) NSAIDs inactivation, (b) activation of pro\u2010drugs, and (c) NSAIDs selectivity. Our assay provides useful information about the selectivity of NSAIDs that could be extended by the analysis of plasma samples taken from humans similarly treated with test drugs.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1999) <jats:bold>126<\/jats:bold>, 1824\u20131830; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0702518\">10.1038\/sj.bjp.0702518<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0702518","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:58:52Z","timestamp":1106942332000},"page":"1824-1830","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":77,"title":["<i>Ex vivo<\/i> assay to determine the cyclooxygenase selectivity of non\u2010steroidal anti\u2010inflammatory drugs"],"prefix":"10.1111","volume":"126","author":[{"given":"Francesco","family":"Giuliano","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Timothy D","family":"Warner","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.2165\/00003495-199300461-00013"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1007\/BF02265118"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.2165\/00003088-199427060-00005"},{"key":"e_1_2_7_5_1","first-page":"1531","article-title":"Pharmacology of a selective cyclooxygenase\u20102 inhibitor, L\u2010745,337: a novel nonsteroidal anti\u2010inflammatory agent with an ulcerogenic sparing effect in rat and nonhuman primate stomach","volume":"274","author":"CHAN C.\u2010C.","year":"1995","journal-title":"J. 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