Description
FR122047 is a selective inhibitor of COX-
1. The IC
50 values for inhibition of human COX-
1 and COX-
2 are 0.028 and 65 μM, respectively. In human platelet-
rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-
induced platelet aggregation with an IC
50 of 180-
200 nM, which is nearly 100 times more potent than aspirin. Unlike aspirin, FR122047 does not induce gastric damage upon oral administration at doses (100 mg/kg) far in excess of the dose needed for complete suppression of platelet COX-
1. In some models of inflammation, such as collagen-
induced arthritis in the rat, FR122047 has an anti-
inflammatory effect, implying a role for COX-
1 in these models.
Biological Activity
Selective cyclooxygenase-1 (COX-1) inhibitor (IC 50 values are 0.028 and 65 μ M for COX-1 and COX-2 respectively). Antiplatelet, analgesic and anti-inflammatory following oral administration in vivo .
References
[1] TAKEHIRO OCHI Toshio G Yukio Motoyama. The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models[J]. European journal of pharmacology, 2000, 391 1: Pages 49-54. DOI:
10.1016/s0014-2999(00)00051-0[2] MIWAKO DOHI . The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor[J]. European journal of pharmacology, 1993, 243 2: Pages 179-184. DOI:
10.1016/0014-2999(93)90378-u[3] TAKEHIRO OCHI Toshio G. Differential effect of FR122047, a selective cyclo-oxygenase-1 inhibitor, in rat chronic models of arthritis[J]. British Journal of Pharmacology, 2009, 135 3: 782-788. DOI:
10.1038/sj.bjp.0704511[4] ANNA-KARIN JOHNSSON . COX-1 dependent biosynthesis of 15-hydroxyeicosatetraenoic acid in human mast cells[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 2021, 1866 5: Article 158886. DOI:
10.1016/j.bbalip.2021.158886
