Interaction of calcium antagonists with cyclic AMP phosphodiesterases and calmodulin

The calcium antagonists, nimodipine and nicardipine, competitively inhibited calmodulin-sensitive and calmodulin-insensitive forms of cyclic AMP phosphodiesterase, with IC 50's in the micromolar range. Verapamil showed similar inhibitory potency against calmodulin-insensitive phosphodiesterases...

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Published inBiochemical and biophysical research communications Vol. 105; no. 3; pp. 1142 - 1149
Main Authors Epstein, Paul M., Fiss, Karen, Hachisu, Reiko, Andrenyak, David M.
Format Journal Article
LanguageEnglish
Published United States Elsevier Inc 01.01.1982
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Summary:The calcium antagonists, nimodipine and nicardipine, competitively inhibited calmodulin-sensitive and calmodulin-insensitive forms of cyclic AMP phosphodiesterase, with IC 50's in the micromolar range. Verapamil showed similar inhibitory potency against calmodulin-insensitive phosphodiesterases, but in marked contrast, it was a very weak inhibitor (30–100 times less potent) against calmodulin-sensitive forms of the enzyme. Verapamil and nimodipine both antagonized the calmodulin stimulation of phosphodiesterase. Through use of hydrophobic fluorescent probes, verapamil, and another calmodulin antagonist, proadifen, were shown to interact directly with calmodulin in a manner that differed from the interaction of calmodulin with trifluoperazine.
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ISSN:0006-291X
1090-2104
DOI:10.1016/0006-291X(82)91089-0