新規ジヒドロピリジン誘導体,塩酸palonidipine(TC-81)の心筋虚血モデル等に対する作用

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概要

• 論文の詳細を見る

• The antianginal effects of palonidipine, a novel 1, 4-dihydropyridine derivative, and nifedipine on various myocardial ischemic models were compared. (1) Palonidipine at 0.5 mg / kg, p.o. significantly inhibited vasopressin-induced ST depression of ECG in Donryu rats. This activity was about 5 times more potent than that of nifedipine and was long-lasting. (2) Palonidipine at 1 mg/kg, i.d. significantly inhibited ST depression induced by isoproterenol in Wistar rats. This activity of TC-81 was more potent than that of nifedipine. (3) Palonidipine at 3 itg/kg, i.v. produced an increase in regional myocardial tissue blood flow in the ischemic region of chronic coronary artery occluded dogs. (4) In isolated dog coronary artery, palonidipine at a concentration of 10-10M or greater inhibited the amplitude of 3, 4-DAP-induced cyclic contractions in a concentration-dependent manner. This activity was 10-30 times more potent than that of nifedipine. (5) An intracoronary injection of endothelin (30pmol/kg) reduced the coronary blood flow, subepicardial tissue blood flow, and subepicardial pH in anesthetized dogs.The ST elevation of ECG over 0.1 mV also occurred in 8 of 10 cases. In all the cases, ventricular extrasystoles were noted, and 9 out of 10 animals died. Pretreatment with palonidipine (3μg/kg, i.v.) inhibited endothelin-induced ischemic changes, with a potency greater than that of nifedipine. These results suggest that palonidipine may be useful for the therapy of angina-pectoris.

• 社団法人 日本薬理学会の論文

著者

• 竹下 徹

  帝人 (株) 医薬開発研究所

• 青木 久美子

  帝人 (株) 医薬開発研究所

• 太田 幹雄

  帝人 (株) 医薬開発研究所

• 岸本 直

  帝人 (株) 医薬開発研究所

• 岡宮 芳明

  帝人 (株) 医薬開発研究所

• 保科 憲二

  帝人 (株) 医薬開発研究所

関連論文

• 新規ジヒドロピリジン誘導体,塩酸palonidipine(TC-81)の心筋虚血モデル等に対する作用
• Effects of clenbuterol on resting tension and contractile response in vesicourethral smooth muscle of rabbits.

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