Timegadine is a competitive inhibitor of COX and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates and in washed rabbit platelets.

Lipo-oxygenase:100 μM (in horse washed rabbit platelets), COX:20 μM (in rat brain), COX:5 nM (in rabbit platelets)

Timegadine is a potent, competitive COX and lipo-oxygenase inhibitor, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets[2],and is a new antiinflammatory agent,

Timegadine is a potent, competitive prostaglandin synthetase inhibitor which also inhibits cyclo-oxygenase (COX) and lipoxygenase. Daily oral doses of 10 to 30 mg/kg of Timegadine significantly inhibit both the primary and secondary lesions of adjuvant arthritis when the treatment is initiated on the day of the disease induction and continues for 28 days. Timegadine is able specifically to prevent the development of the swelling of the non-injected paw until 28 days after the adjuvant injection when administered for 5 days prior to and 5 days after the induction of the disease, in analogy with the effect of cyclophosphamide[1].Timegadine is a new antiinflammatory agent,