Chemical Name:6-(4-Fluorophenyl)-2,3-dihydro-5-(4-pyridinyl)imidazo[2
,1-b]thiazole dihydrochloride
Biological Activity:
Inhibitor of p38 MAP kinase (IC50 =
0.1-1 μM).
Potently inhibits LPS-induced IL-1 and TNF-α production
in human monocytes (IC50 = 1 μM). Also
inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid
metabolism in RBL-1 cells (IC50 values are 10 and 100 μM
respectively). Anti-inflammatory following oral administration in vivo.
Griswoldet al (1987) SK&F 86002: a structurally novel
anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated
metabolism of arachidonic acid. Biochem.Pharmacol. 36 3463. Leeet al (1994) A protein kinase involved in the regulaton of inflammatory
cytokine biosynthesis. Nature 372 739. Nicket al
(1997) Common and distinct intracellular signaling pathways in human
neutrophils utilized by platelet activating factor and FMLP. J.Clin.Invest. 99
975.