WEB 2086 (apafant) is a potent and selective platelet activating (PAF) antagonist. WEB 2086 has high affinity for guinea pig peritoneal macrophage PAF receptors, dissociating slowly. WEB 2086 at 10-8 to 10-6 mol/L strongly and concentration-dependently inhibits PAF-induced chemotaxis in guinea pig eosinophils. In animal models, WEB 2086 (0.1% w/v) blocks eosinophil activation in allergic conjunctivitis and inhibits the hypotensive and lethal effect of PAF in the rat in a dose-related manner.
| Molecular Formula | C22H22ClN5O2S |
| References |
Kato M et al (2004) Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs. J. Pharmacol. Sci. 95:435 Nabe T et al (1997) Eosinophil chemotaxis induced by several biologically active substances and the effects of apafant on it in vitro. Arzneimittel-Forschung 47:1112 Ring et al (1993) Pharmacological characterization of a receptor for platelet-activating factor on guinea pig peritoneal macrophages using [3H]apafant, a selective and competitive platelet-activating factor antagonist: evidence that the noncompetitive behavior of apafant in functional studies relates to slow kinetics of dissociation. Molec. Pharmacol. 43:302 |