Study on new types of calcium antagonists

新型钙拮抗剂的研究

• 批准号: 58870019
• 负责人: HIDAKA Hiroyoshi
• 金额: $ 3.97万
• 依托单位: Mie University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Developmental Scientific Research
• 财政年份: 1983
• 资助国家: 日本
• 起止时间: 1983 至 1985
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-58870019/
• 关键词: calcium antagonist; calmodulin; myosin light chain kinase; MLCK; 【Ca^(2+)】PDE

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.

我们研究了一种新合成的二氮杂吡啶衍生物（CV-159）对钙调素和钙调素激活酶的影响.产生&lt;Ca^（2+）&gt; /钙调蛋白（CaM）激活的肌球蛋白轻链激酶（MLCK）的50%抑制的CV-159浓度为6.2 <micro>M。产生&lt;Ca^（2+）&gt; /CaM激活的环核苷酸磷酸二酯酶（&lt;Ca ^（2+）&gt; -PDE）的50%抑制的CV-159的浓度为0.55 <micro>M。CaM竞争性拮抗CV-159对MLCK和&lt;Ca^（2+）&gt; PDE激活的抑制作用. CV-159对丹磺酰-CaM荧光强度的抑制作用呈依赖性，提示CV-159与其它二氢吡啶类化合物不同，具有CaM拮抗作用。

项目成果

The Journal of Pharmacology and Experimental Therapeutics. 230-3. (1984)

药理学和实验治疗学杂志。

The Proceedings of the 15th Congress of the Japanese Society for Vasoactive Substance Research. 9-1. (1986)

日本血管活性物质研究会第 15 届大会论文集。

J.Pharmacol.Exp.Ther.9-1. (1986)

J.Pharmacol.Exp.Ther.9-1。

The Jouranl of Pharmacology and Experimental Therapeutics. 233-2. (1985)

药理学和实验治疗学杂志。

J.Pharmacol.Exp.Ther.230-3. (1984)

J.Pharmacol.Exp.Ther.230-3。