Stereochemistry | ACHIRAL |
Molecular Formula | C21H19N3O3S |
Molecular Weight | 393.459 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC1=CC=C(C=C1)C2=NN3N=CC=CC3=C2C4=CC=C(C=C4)S(C)(=O)=O
InChI
InChIKey=NXMZBNYLCVTRGB-UHFFFAOYSA-N
InChI=1S/C21H19N3O3S/c1-3-27-17-10-6-16(7-11-17)21-20(19-5-4-14-22-24(19)23-21)15-8-12-18(13-9-15)28(2,25)26/h4-14H,3H2,1-2H3
GW406381 is an investigational, highly selective cyclooxygenase-2 (COX-2) inhibitor for inflammatory pain treatment. It showed effectiveness in animal models of central sensitization such as chronic constriction injury and capsaicin-induced hyperalgesia. It's effect was also evaluated in several clinical trials in patients with peripheral nerve injury (Phase I ), rheumatoid arthritis (Phase III), the signs and symptoms of osteoarthritis of the knee to control of pain and improvement in function (Phase III), and in treating the signs and symptoms of dental pain following third molar tooth extraction (Phase III). Possessing favourable pharmacokinetic profiles and analgesic activity in vivo, GW406381 have also demonstrated relatively high brain penetration in the rat compared with the clinically available compounds, which may ultimately prove beneficial in the treatment of pain.
CNS Activity
Originator
Approval Year
Doses
AEs
Sourcing
PubMed
Sample Use Guides
5mg, 10mg, 25mg, and 50mg administered once daily for 12 weeks in adults with rheumatoid arthritis
Route of Administration:
Oral