WEB-2086 (105219-56-5) is a potent and selective antagonist of the platelet activating factor (PAF) receptor (Ki = 16.3 nM).1 Displays an activity profile which includes antiinflammatory, antiangiogenesis and anticancer activity.2 Along with leukotriene antagonists, WEB-2086 cooperatively provides a robust antiinflammatory effect regulating PMNL migration and edema formation.3 Displays analgesic effects in animal models of neuropathic pain.4 Active in vivo.
1) Dent et al. (1989), Characterization of PAF receptors on human neutrophils using the specific antagonist WEB 2086. Correlation between receptor binding and function; FEBS Lett., 244 365
2) Cellai et al. (2006), Growth inhibition and differentiation of human breast cancer cells by PAFR antagonist WEB-2086; Br. J. Cancer, 94 1637
3) Bitencourt et al. (2013), Cooperative role of endogenous leucotrienes and platelet-activating factor in ischaemia-reperfusion-mediated tissue injury; J. Cell. Mol. Med., 17 1554
4) Motoyama et al. (2013), Pain-releasing action of platelet-activating factor (PAF) antagonists in neuropathic pain animal models and the mechanisms of action; Eur. J. Pain, 17 1156