CV-3988 is a specific antagonist of PAF-R (platelet-activating factor receptor), blocking signaling events correlated to the expression and binding of PAF to the PAF-R (Ki = 0.872 μM). CV-3988 has close structural similarity to PAF allowing recognition by the receptor, where it then associates strongly to the binding site and blocks the activating interaction with PAF. Inhibition of this binding has been used to investigate the numerous cellular consequences of PAF association to the PAF-R. PAF-induced platelet aggregation is inhibited by CV-3988. Mediation of the severity of endotoxin shock was demonstrated upon administration of CV-3988, indicating that PAF serves a pivotal role in the pathogenesis of endotoxin shock. The lethality of anaphylactic shock in mice was also subdued in the presence of CV-3988, suggesting a lethal role of PAF in the anaphylaxis. As a specific antagonist of PAF binding, CV-3988 has seen wide utility as a benchmark PAF-binding antagonist for binding studies with other compounds.
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