Calmodulin antagonists inhibit aggregation of human, guinea pig and rabbit platelets induced with platelet activating factor

FEBS Letters

Levy, Joseph V.¹ 

[1] Pharmacology Laboratories, Kuzell Institute for Arthritis Research, Medical Research Institute, Pacific Medical Center, 2200 Webster Street, San Francisco, CA 94115, USA

关键词: Platelet activating factor;    Calmodulin antagonist;    W-7;    W-5;    Trifluoperazine;    Platelet aggregation;   

DOI  :  10.1016/0014-5793(83)80161-6

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Three calmodulin (CM) antagonists W-7, W-5, and trifluoperazine (TFP) were tested for ability to prevent aggregation of human, guinea pig, and rabbit platelets induced by 7.88 μM PAF. The naphthalene sulfonamide derivatives, W-7 and W-5, were active in all species, W-5 being 1,5–5.7-times less potent than W-7, in accordance with W-5 being a weaker CM inhibitor. ED ₅₀-Values for TFP were 155, 160 and 255 μM for rabbit, human and guinea pig platelets, respectively. Results are consistent with the notion that some substances antagonizing CM may inhibit PAF aggregation effects. W-7 is most effective on human platelets (ED ₅₀ 51.5 μM). High concentrations of TFP required to antagonize PAF-induced aggregation cautions against ascribing its effects solely to an inhibitory effect on CM.

【 授权许可】

Unknown