儿茶酚取代的苯氧基丙醇胺：麻醉猫中的肾上腺素能受体活性
Catechol-substituted phenoxypropanolamines: adrenoceptor activity in the anaesthetized cat.
作者信息
Dowd H, Keh G S, Raper C
出版信息
Br J Pharmacol. 1977 Jun;60(2):197-203. doi: 10.1111/j.1476-5381.1977.tb07741.x.
Abstract
1 The pharmacological actions of racemic noradrenaline, adrenaline, isoprenaline and N-t-butylnoradrenaline have been compared with those of their corresponding derivatives containing an oxymethylene (OXY) link between the ring and ethanolamine side chain. 2 The compounds were tested in the anaesthetized cat for their ability to produce positive chronotropic effects, bronchodilator actions, changes in perfusion pressure in the perfused hind limb and decreases in soleus muscle contractions. 3 All the OXY-derivatives were potent beta-adrenoceptor agonists. The inclusion of the oxymethylene link promotes selectivity for beta1-as opposed to beta2-adrenoceptor activity. 4 In comparison with the parent compounds, the OXY-derivatives of adrenaline and noradrenaline had very weak alpha-adrenoceptor stimulant effects.
摘要
- 已将消旋去甲肾上腺素、肾上腺素、异丙肾上腺素和N-叔丁基去甲肾上腺素的药理作用与其相应的在环与乙醇胺侧链之间含有羟亚甲基（OXY）连接的衍生物的药理作用进行了比较。2. 在麻醉猫中测试了这些化合物产生正性变时作用、支气管扩张作用、灌注后肢灌注压变化以及比目鱼肌收缩减弱的能力。3. 所有的OXY衍生物都是强效的β-肾上腺素能受体激动剂。羟亚甲基连接的存在促进了对β1-而非β2-肾上腺素能受体活性的选择性。4. 与母体化合物相比，肾上腺素和去甲肾上腺素的OXY衍生物具有非常弱的α-肾上腺素能受体刺激作用。
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本文引用的文献
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Eur J Pharmacol. 1967 Dec;2(3):214-23. doi: 10.1016/0014-2999(67)90090-8.
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Use of cumulative dose-response curves in potency comparisons of sympathomimetic amines on the cat soleus muscle.累积剂量-反应曲线在拟交感胺对猫比目鱼肌效能比较中的应用。
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Use of cumulative dose-response curves in potency comparisons of sympathomimetic amines on pulmonary resistance in anaesthesized cats.在麻醉猫中，使用累积剂量-反应曲线比较拟交感胺对肺阻力的效能。
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Cardiac stimulant 1-(hydroxyphenoxy)-3-isopropylamino-2-propanols.心脏兴奋剂1-（羟基苯氧基）-3-异丙氨基-2-丙醇
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Actions of some sympathomimetic bronchodilator and beta-adrenoceptor blocking drugs on contractions of the cat soleus muscle.某些拟交感神经支气管扩张剂和β-肾上腺素能受体阻断药物对猫比目鱼肌收缩的作用。
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