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GW406381 (8), currently undergoing clinical evaluation for the treatment of inflammatory pain is a member of a novel series of 2,3-diaryl-pyrazolo[1,5-b]pyridazine based cyclooxygenase-2 (COX-2) inhibitors, which have been shown to be highly potent and selective. Several examples of the series, in addition to possessing favourable pharmacokinetic profiles and analgesic activity in vivo, 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.

Original publication

DOI

10.1016/j.bmcl.2004.07.089

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/11/2004

Volume

14

Pages

5445 - 5448

Keywords

Administration, Oral, Animals, Arthritis, Experimental, Biological Availability, Brain, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors, Cyclooxygenase Inhibitors, Freund's Adjuvant, Humans, Infusions, Intravenous, Male, Membrane Proteins, Prostaglandin-Endoperoxide Synthases, Pyrazoles, Pyridazines, Rats, Structure-Activity Relationship