Effects of CV-3988, an antagonist of platelet-activating factor (PAF), on washed rabbit platelets.
Platelet-activating factor (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine or AGEPC) is a small, extremely potent phospholipid mediator. CV-3988, a unique structural analogue of AGEPC, has recently been introduced as a selective antagonist of AGEPC-induced in vitro platelet activation and in vivo systemic hypotension. At concentrations greater than 5 X 10(-5) M, CV-3988 itself induced aggregation and secretion responses in washed rabbit platelets. CV-3988 inhibited AGEPC-induced platelet activation at concentrations as low as 10(-8) M, but also blocked platelet activation induced by collagen and calcium ionophore A23187 at concentrations between 10(-6) M and 10(-5) M. The mechanism of inhibition, however, did not depend on increased levels of intracellular 3',5'-cyclic adenosine monophosphate (cAMP). In fact, CV-3988, like AGEPC itself, appeared to lower cAMP levels in washed rabbit platelets.
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D015056:1-Methyl-3-isobutylxanthine / Q000494:pharmacology; D000818:Animals; D001792:Blood Platelets / Q000187:drug effects* / Q000378:metabolism; D000001:Calcimycin / Q000494:pharmacology; D003094:Collagen / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D011464:Epoprostenol / Q000494:pharmacology; D005260:Female; D009994:Osmolar Concentration; D010742:Phospholipid Ethers; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D011817:Rabbits; D013844:Thiazoles / Q000494:pharmacology*
D010742:Phospholipid Ethers; D010972:Platelet Activating Factor; D013844:Thiazoles; D000001:Calcimycin; C037913:CV 3988; D003094:Collagen; D011464:Epoprostenol; D000242:Cyclic AMP; D015056:1-Methyl-3-isobutylxanthine