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犬心脏对盐酸半水合5-(-羟基-2-异丙氨基丁基)-8-羟基喹啉醇(丙卡特罗)、沙丁胺醇、去甲肾上腺素和异丙肾上腺素变时性和变力性反应的比较研究。

Comparative study of chronotropic and inotropic responses to 5-(-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril hydrochloride hemihydrade (procaterol), salbutamol, noradrenaline and isoprenaline in the dog heart.

作者信息

Chiba S

出版信息

Clin Exp Pharmacol Physiol. 1978 Nov-Dec;5(6):601-6. doi: 10.1111/j.1440-1681.1978.tb00715.x.

Abstract
  1. The cardiac chronotropic and inotropic responses to 5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril hydrochloride hemihydrade (procaterol) and salbutamol have been compared to noradrenaline and isoprenaline in isolated blood-perfused canine atrial and ventricular preparations. 2. All four compounds induced dose-related positive chronotropic and inotropic effects, but different individual response patterns were observed. 3. Procaterol and salbutamol were partial agonists compared to noradrenaline and isoprenaline for causing chronotropic and inotropic responses. The order of efficacy for the adrenoceptors mediating both chronotropic and inotropic responses was isoprenaline, noradrenaline, salbutamol and procaterol. The slopes of the salbutamol dose-response curves were flatter than those for isoprenaline and noradrenaline; the slopes of the procaterol dose-response curves were flatter than those for salbutamol. 4. Because of these differences, the order of activity depended upon the level of response chosen for the comparison. When doses producing small chronotropic and inotropic responses were compared, the order of activity was isoprenaline, noradrenaline, procaterol and salbutamol; whereas with doses producing large responses the order was isoprenaline, noradrenaline, salbutamol and procaterol. 5. Procaterol was longer acting than salbutamol, and salbutamol was longer acting than noradrenaline.
摘要
  1. 在离体血液灌注的犬心房和心室标本中,比较了盐酸半水合5-(1-羟基-2-异丙氨基丁基)-8-羟基喹哪啶(丙卡特罗)和沙丁胺醇对心脏变时性和变力性的反应与去甲肾上腺素和异丙肾上腺素的差异。2. 所有四种化合物均诱导出剂量相关的正性变时性和变力性效应,但观察到不同的个体反应模式。3. 与去甲肾上腺素和异丙肾上腺素相比,丙卡特罗和沙丁胺醇在引起变时性和变力性反应方面是部分激动剂。介导变时性和变力性反应的肾上腺素能受体的效能顺序为异丙肾上腺素、去甲肾上腺素、沙丁胺醇和丙卡特罗。沙丁胺醇剂量-反应曲线的斜率比异丙肾上腺素和去甲肾上腺素的更平缓;丙卡特罗剂量-反应曲线的斜率比沙丁胺醇的更平缓。4. 由于这些差异,活性顺序取决于用于比较的反应水平。当比较产生小的变时性和变力性反应的剂量时,活性顺序为异丙肾上腺素、去甲肾上腺素、丙卡特罗和沙丁胺醇;而当比较产生大反应的剂量时,顺序为异丙肾上腺素、去甲肾上腺素、沙丁胺醇和丙卡特罗。5. 丙卡特罗的作用时间比沙丁胺醇长,沙丁胺醇的作用时间比去甲肾上腺素长。

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