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使用新型具有血管舒张活性的正性肌力药物SK&F 94120进行的药理学研究。

Pharmacological studies with SK&F 94120, a novel positive inotropic agent with vasodilator activity.

作者信息

Gristwood R W, Eden R J, Owen D A, Taylor E M

出版信息

J Pharm Pharmacol. 1986 Jun;38(6):452-9. doi: 10.1111/j.2042-7158.1986.tb04609.x.

DOI:10.1111/j.2042-7158.1986.tb04609.x
PMID:2873222
Abstract

The pharmacological properties of SK&F 94120 on the cardiovascular system have been studied in laboratory animal species. The compound was shown to have positive inotropic activity on hearts from guinea-pig, cat, dog and marmoset in-vitro and in cat and dog in-vivo. These responses in-vivo occurred in association with minimal changes in heart rate. Positive inotropic activity was not caused by SK&F 94120 in rat or hamster hearts in-vitro, thereby indicating a species dependence in myocardial response. SK&F 94120 was shown to have vasodilator activity in cats in-vivo. Detailed studies carried out on anaesthetized cats indicated that the compound caused a balanced dilatation of both resistance and capacitance blood vessels. Haemodynamic studies in anaesthetized cats indicated that, as a consequence of the positive inotropic and vasodilator actions, SK&F 94120 causes significant increases in cardiac output and stroke volume. Studies in conscious dogs showed the compound to be active as a positive inotrope after oral administration. The above properties suggest that this compound possesses useful haemodynamic properties for the treatment of congestive heart failure.

摘要

已在实验动物物种中研究了SK&F 94120对心血管系统的药理特性。该化合物在体外对豚鼠、猫、狗和狨猴的心脏以及在体内对猫和狗的心脏均显示出正性肌力活性。这些体内反应伴随着心率的最小变化。体外实验中,SK&F 94120对大鼠或仓鼠心脏未产生正性肌力活性,从而表明心肌反应存在物种依赖性。SK&F 94120在体内对猫显示出血管舒张活性。对麻醉猫进行的详细研究表明,该化合物可使阻力血管和容量血管均衡扩张。对麻醉猫的血流动力学研究表明,由于正性肌力作用和血管舒张作用,SK&F 94120可使心输出量和每搏输出量显著增加。对清醒狗的研究表明,口服给药后该化合物作为正性肌力药物具有活性。上述特性表明,该化合物具有治疗充血性心力衰竭的有用血流动力学特性。

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