CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor, inhibiting aggregation of rabbit and human platelets induced by PAF with IC values of 75 and 170 nM, respectively. It has little action on platelet aggregation induced by arachidonic acid, ADP, or collagen. CV-6209 is bioavailable, as it prevents PAF-induced hypotension in rats, while not blocking hypotension triggered by arachidonic acid , histamine, bradykinin , or isoproterenol . CV-6209 is used to study the role of PAF receptor signaling in vitro and in vivo.
CV-6209 is a potent antagonist of platelet activating factor (PAF). CV-6209 inhibits the PAF-induced aggregation of rabbit and human platelets, with IC50s of 75 nM and 170 nM, respectively. CV-6209 can inhibit PAF-induced hypotension in rats[1].
体外研究
CV-6209 inhibits [3H]serotonin release from rabbit platelets stimulated with PAF (30 nM)[1] .
CV-6209 has little action on platelet aggregation induced by arachidonic acid, ADP, or collagen[1] .
CV-6209 (0.2-2 μM; pretreated for 30 min) inhibits PAF-induced MC degranulation in both LAD2 and hLMCs[1].
体内研究
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[1] .