Characterization of the activity of a platelet activating factor antagonist, CV-3988.
CV-3988 inhibited the vascular permeability increase induced by C16-PAF and C18-PAF in rat skin in a dose-dependent manner. The inhibition was shown to be specific and competitive with PAF on its receptor by the following observations: parallel shift of the dose-response curve; crossing of double reciprocal plots on the intersection of the ordinate; and no inhibition on other autacoids such as bradykinin, histamine, 5-hydroxytryptamine and LTC4. PAF-induced blood pressure fall in rats was also suppressed by pretreatment with CV-3988 selectively.
D000525:Alprazolam / Q000494:pharmacology; D000818:Animals; D012898:Autacoids / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects*; D002199:Capillary Permeability / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D008297:Male; D010742:Phospholipid Ethers; D010972:Platelet Activating Factor / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors*; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012867:Skin / Q000098:blood supply; D013844:Thiazoles / Q000494:pharmacology*
D012898:Autacoids; D010742:Phospholipid Ethers; D010972:Platelet Activating Factor; D013844:Thiazoles; C037145:1-hexadecyl-2-acetyl-glycero-3-phosphocholine; C037913:CV 3988; C026613:1-0-octadecyl 2-0-acetyl sn-glycero-3-phosphorylcholine; D000525:Alprazolam