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“选择性”β-肾上腺素能受体阻断药物对心肌循环的影响。

The effect of "selective" beta-adrenoceptor blocking drugs on the myocardial circulation.

作者信息

Parratt J R, Wadsworth R M

出版信息

Br J Pharmacol. 1970 Jun;39(2):296-308. doi: 10.1111/j.1476-5381.1970.tb12893.x.

Abstract
  1. A comparison has been made of the effects of a relatively specific beta(1)-adrenoceptor blocking drug (practolol) and a relatively specific beta(2)-adrenoceptor blocking drug (butoxamine) on myocardial and general haemodynamics in anaesthetized cats.2. Practolol, in a dose (10 mg/kg, intravenously) which had little effect on arterial pressure, heart rate, myocardial blood flow or myocardial vascular resistance, markedly reduced the effects of isoprenaline infusions on heart rate, aortic dp/dt, myocardial blood flow, vascular resistance and metabolic heat production, and the cardiac effort index. Isoprenaline induced vasodepression was unaffected.3. Butoxamine (5 mg/kg, intravenously) decreased heart rate, aortic dp/dt, the cardiac effort index and myocardial blood flow and increased myocardial vascular resistance. This is taken as further evidence for the existence of beta(2)-adrenoceptors in the myocardial microcirculation.4. After butoxamine, the effects of isoprenaline on myocardial blood flow, myocardial vascular resistance and heart rate were unaffected but the peripheral vasodilator effect was abolished. The effects on aortic dp/dt and the cardiac effort index were potentiated.5. It is concluded that the effect of isoprenaline in increasing myocardial blood flow is due predominantly to increased cardiac work and oxygen consumption and that practolol, since it has little direct effect on myocardial blood flow yet abolishes the cardiac stimulant and oxygen wasting effects of released catecholamines, has properties which indicate that it should be an effective and safe anti-anginal drug.
摘要
  1. 已对一种相对特异性的β₁肾上腺素能受体阻断药物(心得宁)和一种相对特异性的β₂肾上腺素能受体阻断药物(丁氧胺)对麻醉猫心肌和全身血流动力学的影响进行了比较。

  2. 心得宁静脉注射剂量为10mg/kg时,对动脉压、心率、心肌血流量或心肌血管阻力几乎没有影响,但能显著降低异丙肾上腺素输注对心率、主动脉dp/dt、心肌血流量、血管阻力和代谢产热以及心脏作功指数的影响。异丙肾上腺素引起的血管减压作用未受影响。

  3. 丁氧胺(静脉注射5mg/kg)可降低心率、主动脉dp/dt、心脏作功指数和心肌血流量,并增加心肌血管阻力。这被视为心肌微循环中存在β₂肾上腺素能受体的进一步证据。

  4. 丁氧胺给药后,异丙肾上腺素对心肌血流量、心肌血管阻力和心率的影响未受影响,但外周血管舒张作用被消除。对主动脉dp/dt和心脏作功指数的影响增强。

  5. 得出结论,异丙肾上腺素增加心肌血流量的作用主要归因于心脏作功和氧消耗的增加,而心得宁由于对心肌血流量几乎没有直接影响,但能消除释放的儿茶酚胺的心脏刺激和氧消耗作用,其特性表明它应该是一种有效且安全的抗心绞痛药物。

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Cardioselective beta-adrenergic blockade.心脏选择性β-肾上腺素能阻断
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本文引用的文献

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Myocardial blood flow in the rabbit.兔子的心肌血流量。
Am J Physiol. 1961 May;200:968-74. doi: 10.1152/ajplegacy.1961.200.5.968.
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An analysis of selective beta receptor blockade.选择性β受体阻断作用分析
Eur J Pharmacol. 1969 Feb;5(3):227-34. doi: 10.1016/0014-2999(69)90142-3.

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