1985 Fiscal Year Final Research Report Summary
Study on new types of calcium antagonists
| Project/Area Number |
58870019
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| Research Category |
Grant-in-Aid for Developmental Scientific Research
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| Allocation Type | Single-year Grants |
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| Research Field |
薬理学(基礎薬理学,臨床薬理学,中毒学等)
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| Research Institution | Mie University |
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Principal Investigator |
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| Project Period (FY) |
1983 – 1985
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| Keywords | calcium antagonist / calmodulin / myosin light chain kinase / MLCK / 【Ca^(2+)】PDE |
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| Research Abstract |
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.
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