Summary
WEB 2086 is a novel PAF-acether antagonist, whose pharmacological action in man has only been preliminarily defined. Twelve healthy male volunteers received oral doses of 5, 30 and 90 mg and over the following 24 h inhibition of 5 × 10−8 M PAF-acether-induced platelet aggregation ex vivo was studied as an indicator of pharmacological activity.
WEB 2086 inhibited PAF-acether-induced platelet aggregation in all the doses tested, with the maximum effect 1 to 2 h after administration. After 2 h 5- 30- and 90-mg doses caused, respectively, 87, 98 and 100% inhibition. The magnitude and duration of the inhibitory effect was dose-dependent, with a significant action still detectable 10 h after administration of all three doses, and 12 h after administration of the two highest doses (30 and 90 mg).
The subjects did not complain of any significant adverse effect and all completed the study.
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Admaus, W.S., Heuer, H., Meade, C.J. et al. Inhibitory effect of oral WEB 2086, a novel selective PAF-acether antagonist, on ex vivo platelet aggregation. Eur J Clin Pharmacol 35, 237–240 (1988). https://doi.org/10.1007/BF00558259
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DOI: https://doi.org/10.1007/BF00558259