Spasmolytic Effect of Efonidipine Hydrochloride in Isolated Canine Coronary Artery : Comparison with the Effects of Nifedipine and Nisoldipine

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概要

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• Spasmolytic effects of efonidipine hydrochloride (efonidipine) on high K^+-, U46619- and 3,4-diaminopyridine (3,4-DAP)-induced contractions were evaluated in isolated canine coronary artery, and were compared with the effects of nifedipine and nisoldipine. Efonidipine (0.3-30 nM), nifedipine (1-300 nM) and nisoldipine (0.1-100 nM) each relaxed the contractions induced by high K^+ and U46619. However, relaxation produced by efonidipine was slower than that produced by nifedipine or nisoldipine. The rank order of potency of these drugs for U46619-induced contraction was efonidipine ≥ nisoldipine > nifedipine, whereas in high K^+-induced contraction, it was nisoldipine > efonidipine > nifedipine. Thus, the relaxing effect of efonidipine on U46619-induced contraction appeared to be more potent than its effect on high K^+-induced contractions, when compared with the effects of nifedipine and nisoldipine. These three drugs also suppressed 3,4-DAP-induced rhythmic contractions. However, a marked time-dependent increase in potency was only observed for efonidipine, and was similar to its time-dependent effect on high K^+- and U46619-induced contractions. Efonidipine did not change the contraction cycle length whilst suppressing the peak contractions. On the other hand, lower concentration of nifedipine at 3 nM and nisoldipine at 1 nM significantly shortened the cycle length. These results suggest that efonidipine may be an effective agent for the treatment of angina pectoris. The high potency of efonidipine for U46619-induced contractions will provide some advantages in the clinical use of this compound on thromboxane A_2-mediated coronary vasoconstriction.

• 公益社団法人日本薬学会の論文
• 1997-02-15

著者

• KURIMOTO Tadashi

  Central Rsearch Laboratories, Zeria Pharmaceutical Co., Ltd.

• FUKUDA Yoichi

  Central Research Institute, Fuji Oil Co.

• TAMAKI Hajime

  Laboratories of Applied Biochemistry, Faculty of Agriculture, University of the Ryukyus

• HIGASHINO Raita

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.

• TAMAKI Hajime

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.,

• Fukuda Y

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• Tamaki Hajime

  The Third Department Of Internal Medicine Tokyo Medical And Dental University

• Tamaki Hajime

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• Tamaki Hajime

  Chemistry And Technology Of Plant Products Laboratory Kobe University

• Sato Ryuichi

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• JIN Hiromasa

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.

• Jin Hiromasa

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• Higashino R

  Central Research Laboratories Zeria Pharmaceutical Co. Ltd.

• Kurimoto T

  Zeria Pharmaceutical Co. Ltd. Saitama Jpn

• Kurimoto Tadashi

  Central Rsearch Laboratories Zeria Pharmaceutical Co. Ltd.

• 福田 陽一

  Kyoto Pharmaceutical University

• 福田 陽一

  小城製薬株式会社研究所

• KURIMOTO Tadashi

  Central Research Laboratories, Zeria Pharmaceutical Co., Ltd.

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