| Japanese |
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| Title | 選択的エンドセリンETA受容体拮抗薬BQ-485の冠循環への効果 ―その心保護薬としての可能性に関する検討― |
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| Subtitle | 原著 |
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| Authors | 佐久間一郎, 浅島弘志, 北畠顕 |
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| Organization | 北海道大学医学部循環器内科 |
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| Journal | 循環制御 |
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| Volume | 16 |
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| Number | 3 |
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| Page | 377-381 |
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| Year/Month | 1995/ |
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| Article | 原著 |
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| Publisher | 日本循環制御医学会 |
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| Abstract | 「要旨」エンドセリン(ET-1およびET-3, 10pmol)投与は, ラット摘出心の冠血管床を一過性に拡張させ, その後持続的に収縮させる. この作用に対するETA選択的拮抗薬の効果について検討した. 本実験系において冠血管をサポニン処理すると, ETによる冠拡張作用は消失し, 収縮作用が著しく増強した. 選択的ETA受容体拮抗薬BQ-485(1μM)は, ET-1による拡張持続時間を有意に延長させ, 収縮作用減少させた. 同薬はサポニン処理後のET-1による冠血管収縮作用を抑制した. 以上より, 内皮細胞障害時にET-1がETA受容体に介して心筋灌流を悪化させる可能性, および選択的ETA拮抗薬がそれを予防する可能性が示唆された. |
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| Practice | 基礎医学・関連科学 |
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| Keywords | Endothelin, BQ-485, Endothelium-derived relaxing factor (EDRF) Rat, Coronary vascular beds |
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| English |
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| Title | Possible Role of the Selective Endothelin ETA Receptor Antagonist BQ-485 on Cardioprotection |
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| Subtitle | |
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| Authors | Ichiro Sakuma, Hiroshi Asajima, Akira Kitabatake |
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| Authors(kana) | |
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| Organization | Department of Cardiovascular Medicine, Hokkaido University School of Medicine |
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| Journal | Circulation Control |
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| Volume | 16 |
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| Number | 3 |
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| Page | 377-381 |
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| Year/Month | 1995/ |
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| Article | Original article |
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| Publisher | Japan Society of Circulation Control |
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| Abstract | We aimed to assess the effects of BQ-485, a selective endothelin (ET) A (ETA) receptor antagonist, on the vasomotion induced by a low dose of ET. In the isolated rat heart perfused at a constant flow with Krebs-Henseleit solution the intracoronary bolus injection of ET-1 or ET-3 (10 pmol) elicited a rapid transient decrease, followed by a sustained increase, in the coronary perfusion pressure (CPP). The decrease in CPP induced by ET-1 was shorter than that by ET-3. Pretreatment of the heart with saponin (30 mg/ml) to denude the coronary endothelium abolished the decrease and markedly enhanced the increase in CPP induced by ETs. The selective ETA receptor antagonist BQ-485 (1 mM) significantly prolonged the ET-1-induced decrease in CPP, and eliminated the subsequent increase in CPP. In the saponin treated heart, BQ-485 potently inhibited the ET-1-mediated increase in CPP. It is thus suggested that in the rat coronary vascular beds the low dose ET-1 induces a vasoconstriction and an endothelium-dependent vasodilatation through ETA receptors on the vascular smooth muscle and ETB receptors on the endothelium, respectively. Furthermore, it would be expected that selective ETA receptor antagonists including BQ-485 are able to protect heart against the ET-1-induced coronary vasospasm in the diseased conditions such as atherosclerosis, diabetes melitus or hyperlipidemia in which the release and/or function of endothelium-derived relaxing factors have been reported to be impaired. (Circ Cont 16：377〜381, 1995) |
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| Practice | Basic medicine |
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| Keywords | Endothelin, BQ-485, Endothelium-derived relaxing factor (EDRF) Rat, Coronary vascular beds |
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