A new Ca-antagonist, CD-349, binding to the Ca-channel of rat myocardium and brain and hog coronary artery.

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概要

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• The binding to a Ca-channel of a novel 1, 4-dihydropyridine (DHP) Ca-antagonist, 2-nitratopropyl 3-nitratopropyl 2, 6-dimethyl-4-(3-nitrophenyl)-1, 4-dihydropyridine-3, 5-dicarboxylate (CD-349), was studied in rat myocardium and brain and hog coronary artery, and the binding was compared with that of other DHPs. In rat myocardium, the binding reaction of [<SUP>3</SUP>H]CD-349 was faster than that of nitrendipine (NTD). The association rate constant of [<SUP>3</SUP>H]CD-349 was about 10 times higher than that of [<SUP>3</SUP>H] NTD. The dissociation rate was also higher than that of [<SUP>3</SUP>H]NTD. Scatchard plot analysis of [<SUP>3</SUP>H]CD-349 binding showed one high affinity site for CD-349. The dissociation constant (K<SUB>d</SUB>) and maximum number of binding sites (B<SUB>max</SUB>) were 333 pM and 286 fmoles/mg protein. They were almost the same as those for [<SUP>3</SUP>H]NTD. [<SUP>3</SUP>H]CD-349 and [<SUP>3</SUP>H]NTD bindings were dose dependently inhibited by 1, 4-DHPs: nifedipine, nimodipine, nicardipine and CD-349. The order of the inhibitory potency of these drugs was CD-349>nicardipine>nimodipine>nifedipine, when [<SUP>3</SUP>H]CD-349 and [<SUP>3</SUP>H]NTD were used as the ligands. Similar results were obtained for rat brain and hog coronary artery. [<SUP>3</SUP>H]-CD-349 binding was not changed by α- or β-adrenergic, cholinergic, histaminergic or serotonergic agents in rat myocardium. From these results, it is suggested that CD-349 binds to the Ca-channel reversibly with high affinity due to its high association rate for the site.

• 公益社団法人 日本薬理学会の論文

著者

• Aihara Hironaka

  Research Center Taisho Pharmaceutical Co. Ltd.

• Muramatsu Makoto

  Research Center Taisho Pharmaceutical Co. Ltd.

• ISHII Yumi

  Research Center, Taisho Pharmaceutical Co., Ltd.

• TANAKA Makoto

  Research Center, Taisho Pharmaceutical Co., Ltd

• FUJITA-TOMINAGA Atsuko

  Research Center, Taisho Pharmaceutical Co., Ltd.

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