|show drug details|
|Acetic acid, (o-(2,6-dichloro-4-hydroxyanilino)phenyl)-|
|Benzeneacetic acid, 2-((2,6-dichloro-4-hydroxyphenyl)amino)-|
|Benzeneacetic acid, 2-[(2,6-dichloro-4-hydroxyphenyl)amino]-|
|Ki: ||Kd:||Ic 50:||Ec50/Ic50:|
Aceclofenac blocks prostaglandin E2 production following its intracellular conversion into cyclooxygenase inhibitors.. R Yamazaki; S Kawai; T Matsuzaki; N Kaneda; S Hashimoto; T Yokokura; R Okamoto; T Koshino; Y Mizushima (1997) European journal of pharmacology display abstract
Aceclofenac, 2-[(2,6-dichlorophenyl) amino] phenylacetoxyacetic acid, is a novel non-steroidal anti-inflammatory drug. We investigated the effects of aceclofenac on prostaglandin E2 production by several kinds of human cells. Aceclofenac inhibited interleukin-1beta-induced prostaglandin E2 production by human rheumatoid synovial cells, but had no inhibitory effect on cyclooxygenase-1 or cyclooxygenase-2 activities by itself. We also observed that part of the aceclofenac was converted into diclofenac, the cyclooxygenase-1 and cyclooxygenase-2 inhibitor, when aceclofenac was incubated with human rheumatoid synovial cells. Aceclofenac was also converted into diclofenac and 4'-hydroxy diclofenac by human polymorphonuclear leukocytes and monocytes. 4'-Hydroxy diclofenac suppressed prostaglandin E2 production specifically by blocking cyclooxygenase-2 activity. These findings suggested that aceclofenac can be metabolized to cyclooxygenase inhibitors (diclofenac and/or 4'-hydroxy diclofenac) by these inflammatory cells. Although detailed examinations in non-inflammatory cells remain to be studied, we concluded that aceclofenac is shown to be a new type of non-steroidal anti-inflammatory drug which is intracellulary converted into active metabolites that inhibit the prostaglandin E2 production.