CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor, inhibiting aggregation of rabbit and human platelets induced by PAF with IC50 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.