In Vitro: CV-6209 inhibits [3H]serotonin release from rabbit platelets stimulated with PAF (30 nM). CV-6209 has little action on platelet aggregation induced by arachidonic acid, ADP, or collagen. CV-6209 (0.2-2 μM; pretreated for 30 min) inhibits PAF-induced MC degranulation in both LAD2 and hLMCs.
In Vivo: CV-6209 (i.v.) inhibits PAF (0.3 μg/kg; i.v.)-induced hypotension in rats (ED50=0.009 mg/kg) with no effect on the hypotension induced by arachidonic acid, histamine, bradykinin and isoproterenol. CV-6209 (66 μg; i.v.) reduces asparaginase-induced hypersensitivity compared with nonpretreated, sensitized mice.