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新型钙拮抗剂莫那普利(AJ-2615)在实验性心律失常模型中的抗心律失常作用[校正后]

Anti-arrhythmic effects of a new calcium antagonist, monatepil, AJ-2615, in experimental arrhythmic models [corrected].

作者信息

Yamamoto T, Hosoki K, Karasawa T

机构信息

Department of Pharmacology, Dainippon Pharmaceutical Co. Ltd, Osaka, Japan.

出版信息

Clin Exp Pharmacol Physiol. 1993 Jul-Aug;20(7-8):497-500. doi: 10.1111/j.1440-1681.1993.tb01731.x.

Abstract
  1. To characterize the anti-arrhythmic properties of a new calcium antagonist, monatepil [corrected], AJ-2615, the preventive effects of AJ-2615 were compared with those of the existing calcium antagonists, diltiazem and verapamil, in experimental models of arrhythmia. 2. AJ-2615 (0.1-3.0 mg/kg, i.v.) suppressed ventricular arrhythmias induced by adrenaline (10 micrograms/kg, i.v.) in rats. AJ-2615 (0.1 mg/kg per min for 2 min, i.v.) also suppressed atrial tachycardia induced by aconitine (0.01% aconitine solution) in rats. 3. In these activities, AJ-2615 was comparable to or more potent than diltiazem and verapamil which are widely used for the treatment of arrhythmia. 4. In pro-arrhythmic activity, AJ-2615 was less potent than diltiazem and verapamil. 5. These results suggest that AJ-2615 would be a safer anti-arrhythmic agent, with less proarrhythmic liability than diltiazem and verapamil.
摘要
  1. 为了表征新型钙拮抗剂莫那地尔(已校正,AJ - 2615)的抗心律失常特性,在心律失常实验模型中,将AJ - 2615的预防效果与现有钙拮抗剂地尔硫䓬和维拉帕米的预防效果进行了比较。2. AJ - 2615(0.1 - 3.0毫克/千克,静脉注射)可抑制大鼠体内由肾上腺素(10微克/千克,静脉注射)诱发的室性心律失常。AJ - 2615(0.1毫克/千克每分钟,持续2分钟,静脉注射)也可抑制大鼠体内由乌头碱(0.01%乌头碱溶液)诱发的房性心动过速。3. 在这些活性方面,AJ - 2615与广泛用于治疗心律失常的地尔硫䓬和维拉帕米相当或更有效。4. 在促心律失常活性方面,AJ - 2615比地尔硫䓬和维拉帕米的活性低。5. 这些结果表明,AJ - 2615可能是一种更安全的抗心律失常药物,与地尔硫䓬和维拉帕米相比,其促心律失常风险更低。

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