Study on new types of calcium antagonists

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We examined the effects of a newly synthesized dihydrophridine derivative (CV-159) on calmodulin and calmodulin-activated enzymes.1. The concentration of CV-159 producing 50% inhibition of <Ca^(2+)> /calmodulin (CaM) activated myosin light chain kinase (MLCK) was 6.2 <micro> M.2. The concentration of CV-159 producing 50% inhibition of <Ca^(2+)> /CaM activated cyclic nucleotide phosphodiesterase ( <Ca^(2+)> -PDE) was 0.55 <micro> M.3. CaM antagonized competitively the CV-159-induced inhibition of activation of both MLCK and <Ca^(2+)> PDE.4. CV-159 produced a decrease in dansyl-CaM fluorescence intensity in a <Ca^(2+)> -dependent fashion.These results suggest that CV-159 is different from the other dihydropyridine derivatives, has CaM antagonistic action.