The pharmacological profile of CGP 28238, a highly potent anti-inflammatory compound

Overview of COX-2 in inflammation: from the biology to the clinic

“…Flosulide exhibited potent anti-inflammatory activity in rat adjuvant arthritis with improved gastrointestinal tolerability when compared with standard NSAIDs [133]. A selective inhibition of COX-2 was also later found in several in vitro assays [120,125,132,[134][135][136].…”

Structural diversity of selective COX-2 inhibitors

“…8) led to a renewed interest in this general class of anti-inflammatory agents [16,95,96]. Likewise, the nonulcerogenic anti-inflammatory activity of nimesulide [94] and the close structural analog flosulide [97] had been previously established, but re-evaluation of both compounds as COX inhibitors revealed their selective COX-2 inhibitory properties [98]. The common structural features of the alkylsulfonanilides are depicted in Figure 8.…”

Inhibition of interleukin-1 (IL-1) enhanced pain reflexes in the rabbit by CGP 28238

“…In this species, CGP 28238 inhibits prostaglandin (PG) production more effectively in inflamed tissues than in the gastro-intestinal mucosa [1]. To further investigate the hypothesis of tissue-or stimulus-specific inhibition of PG synthesis, we have compared the effects of CGP28238 and indomethacin on bradykinin induced pain reflexes and on IL-I enhanced acetylcholine induced pain reflexes and PGE 2 production in the isolated perfused rabbit ear model.…”