A NSAID and COX-2 inhibitor
GW 406381 is a non-steroidal anti-inflammatory drug (NSAID) and COX-2 inhibitor (IC50 = 3 nM).1 It is selective for COX-2 over COX-1 (IC50 = >84.2 ?M). GW 406381 (5 mg/kg) reverses chronic construction injury-induced decreases in paw withdrawal thresholds in a rat model of neuropathic pain.2
1.Beswick, P., Bingham, S., Bountra, C., et al.Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitorsBioorg. Med. Chem. Lett.14(21)5445-5448(2004) 2.Zhao, F.-Y., Spanswick, D., Martindale, J.C., et al.GW406381, a novel COX-2 inhibitor, attenuates spontaneous ectopic discharge in sural nerves of rats following chronic constriction injuryPain128(1-2)78-87(2007)
动态评分
0.0