Antianginal Effects of Lercanidipine on the Vasopressin or Methacholine Induced Anginal Model in Rats(Pharmacology)

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概要

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• The antianginal effects of lercanidipine, a newly synthesized 1,4-dihydropyridine derivative calcium channel antagonist, were evaluated in experimental angina model rats and the effects were compared with those of nifedipine, benidipine and amlodipine. In the vasopressin-induced angina model, intravenous administration of lercanidipine dose-dependently suppressed vasopressin-induced ST-depression. Amlodipine barely suppressed it, while benidipine, at the same dose, completely suppressed it. Nifedipine had a potency between that of amlodipine and benidipine. Oral administration of lercanidipine showed similar effects to the intravenous administration test on ST change. High doses of amlodipine, benidipine and nifedipine suppressed ST-depression by almost 100%. In the methacholine-induced angina model, lercanidipine suppressed the ST elevation dose dependently. Amlodipine barely suppressed it, while benidipine at 30μg/kg effected almost total suppression. Nifedipine had a potency between that of amlodipine and benidipine. Intraduodenal administration of lercanidipine also suppressed the ST-elevation dose dependently. Nifedipine, benidipine and amlodipine at 10 mg/kg all markedly suppressed the elevation. Lercanidipine was more potent than the other calcium channel antagonists tested. In conclusion, it was explicitly demonstrated that lercanidipine exerts potent protective effects on the ischemic electrocardiography (ECG) changes in a variety of putative angina pectoris models in rats. An antispasmolytic coronary vasodilating action may be involved in the mechanism. It is expected that lercanidipine will be useful as an antianginal agent.

• 社団法人日本薬学会の論文
• 2005-05-01

著者

• 油田 正樹

  Medicinal Evaluation Laboratory Tsumura Research Institute

• Kase Y

  Tsumura Research Laboratories Tsumura & Co.

• Kase Yoshio

  ツムラ漢方生薬研究所

• Kase Yoshio

  国立長寿医療センター研究所 老年病研究部

• Kase Yoshio

  Central Research Laboratory Tsumura & Co.

• Aburada M

  Fac. Of Pharmacy Musashino Univ.

• Aburada M

  Tsumura Research Inst. Pharmacology Ibaraki Jpn

• 加瀬 義夫

  津村薬理研究所

• KASE Yoshio

  Medicinal Evaluation Laboratory, Tsumura & Co.

• TAKEDA Shuichi

  Medicinal Evaluation Laboratory, Tsumura & Co.

• ABURADA Masaki

  Medicinal Evaluation Laboratory, Tsumura & Co.

• SASAKI Toshinobu

  Medicinal Evaluation Laboratory, Research Division, Tsumura & Co.

• MARUYAMA Hirofumi

  Medicinal Evaluation Laboratory, Research Division, Tsumura & Co.

• 竹田 秀一

  Tsumura & Co. Tsumura Res. Laboratories

• 油田 正樹

  ツムラ研究本部 医薬評価研究所

• Kase Yoshio

  ツムラツムラ研究所

• Aburada Masaki

  Musashino Univ. Tokyo Jpn

• Sasaki Toshinobu

  Medicinal Evaluation Laboratory Research Division Tsumura & Co.:division Of Medicinal Informatic

• Maruyama Hirobumi

  Tsumura Research Laboratories Tsumura & Co.

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