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Calmodulin antagonists inhibit aggregation of human, guinea pig and rabbit platelets induced with platelet activating factor
Author(s) -
Levy Joseph V.
Publication year - 1983
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(83)80161-6
Subject(s) - trifluoperazine , platelet , guinea pig , platelet activating factor , calmodulin , ed50 , chemistry , pharmacology , platelet aggregation , biochemistry , in vitro , biology , endocrinology , immunology , enzyme
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.