A prodrug form of valdecoxib
Parecoxib Sodium (SC 69124A) is a potent and selective COX-2 inhibitor.IC50 value:Target: COX-2in vitro: The prodrug Parecoxib as well as its active metabolite val have a specific affinity to the cannabinoid (CB) receptor measured in CB1-expressing HEK 293 cells and rat brain tissue [1].in vivo: Adult male Sprague-Dawley rats were administered parecoxib (10 or 30 mg kg(-1), IP) or isotonic saline twice a day starting 24 h after middle cerebral artery occlusion (MCAO) for three consecutive days [2]. The selective COX-2 inhibitor parecoxib was delivered 20 min before or 20 min after the incision by intraperitoneal injection. Pretreatment with parecoxib markedly attenuated the pain hypersensitivity induced by incision [3].
参考文献:
[1]. Schreder H, et al. Parecoxib and its metabolite valdecoxib directly interact with cannabinoid binding sites in CB1-expressing HEK 293 cells and rat brain tissue. Neurochem Int. 2011 Jan;58(1):9-13.
[2]. Ye Z, et al. Delayed administration of parecoxib, a specific COX-2 inhibitor, attenuated postischemic neuronal apoptosis by phosphorylation Akt and GSK-3β. Neurochem Res. 2012 Feb;37(2):321-9.
[3]. Guo YJ, et al. Analgesic effects of the COX-2 inhibitor parecoxib on surgical pain through suppression of spinal ERK signaling. Exp Ther Med. 2013 Jul;6(1):275-279.
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