Description
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
50 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.
Chemical Properties
Pale-Yelow Solid
Uses
Competitive PAF receptor antagonist. Inhibits PAF induced human platelet aggregation. Inhibits PAF induced hypotension and lethality.
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[1].
CV-6209 (66 μg; i.v.) reduces asparaginase-induced hypersensitivity compared with nonpretreated, sensitized mice[3].
References
[1] Z TERASHITA. CV-6209, a highly potent antagonist of platelet activating factor in vitro and in vivo.[J]. Journal of Pharmacology and Experimental Therapeutics, 1987, 242 1: 263-268.
[2] H. S. LEONG. Vimentin autoantibodies induce platelet activation and formation of platelet-leukocyte conjugates via platelet-activating factor[J]. Journal of Leukocyte Biology, 2007, 83 2: 263-271. DOI:
10.1189/jlb.0607339[3] SILVIA MUSIO. Anaphylaxis to a self-peptide in the absence of mast cells or histamine[J]. Laboratory Investigation, 2009, 89 4: 398-405. DOI:
10.1038/labinvest.2009.4
