Effects of KB-2796, a new calcium antagonist, and other diphenylpiperazines on (3H)nitrendipine binding.

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概要

• 論文の詳細を見る

• The effect of KB-2796, a new diphenylpiperazine calcium antagonist, on [<SUP>3</SUP>H]nitrendipine ([<SUP>3</SUP>H]NTD) binding was investigated in synaptosomal membranes prepared from the guinea pig cerebral cortex. KB-2796 inhibited [<SUP>3</SUP>H] NTD binding in a dose-dependent manner with an IC50 value of 86 nM. In this respect, KB-2796 was the most potent among the diphenylpiperazine derivatives tested. Saturation binding data indicated that this inhibition resulted from a decrease in the binding affinity without changes in the maximal number of binding sites. KB-2796, however, significantly increased the dissociation rate constant of [<SUP>3</SUP>H] NTD from radiolabeled membranes. This finding suggests that KB-2796 inhibits [<SUP>3</SUP>H]-NTD binding by a negative heterotropic allosteric mechanism. Other diphenyl-piperazines tested also showed similar inhibitory properties. Diphenylpiperazines may act at a site, which is different from the 1, 4-dihydropyridine binding site, on the voltage-dependent calcium channel.

• 公益社団法人 日本薬理学会の論文

著者

• Ito Keizo

  Pharmaceuticals Research Center Kanebo Ltd.

• OHTAKA HIROSHI

  Pharmaceuticals Research Center, Kanebo Ltd.

• KANAZAWA TOSHIRO

  Pharmaceuticals Research Center, Kanebo Ltd.

• IWAMOTO Takahiro

  Pharmaceuticals Research Center, Kanebo, Ltd.

• MORITA Tominori

  Pharmaceuticals Research Center, Kanebo, Ltd.

• KANAZAWA Toshiro

  Pharmaceuticals Research Center, Kanebo, Ltd.

• OHTAKA Hiroshi

  Pharmaceuticals Research Center, Kanebo, Ltd.

• ITO Keizo

  Pharmaceuticals Research Center, Kanebo, Ltd.

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• Effects of KB-2796, a new calcium antagonist, and other diphenylpiperazines on (3H)nitrendipine binding.

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