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Relationship between structure of phenothiazine analogues and their activity on platelet calcium fluxes
Author(s) -
Enouf J.,
LévyToledano S.
Publication year - 1984
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1984.tb10104.x
Subject(s) - trifluoperazine , ionophore , phenothiazine , calmodulin , calcium , vesicle , chemistry , chlorpromazine , platelet , biophysics , biochemistry , membrane , pharmacology , biology , immunology , organic chemistry
1 Phenothiazine analogues have been tested for their effect on calcium uptake into platelet membrane vesicles and on ionophore‐induced platelet activation, both phenomena being Ca 2+ ‐dependent. 2 Both calcium uptake into membrane vesicles and ionophore‐induced platelet activation were inhibited by the drugs. 3 Evidence for two inhibitors as potent as chlorpromazine and trifluoperazine was found. 4 These drugs are apparently competitive inhibitors of calcium uptake. 5 A structure‐activity relationship has been established. 6 The data suggest that the phenothiazines are able to inhibit calmodulin‐insensitive calcium uptake of platelet membrane vesicles and that therefore they cannot be assumed to be selective inhibitors of calmodulin interactions under all circumstances.