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AQ 110与异丙肾上腺素和沙丁胺醇心血管作用的比较。

A comparison of the cardiovascular actions of AQ 110 with those of isoprenaline and salbutamol.

作者信息

Fogelman F, Grundy H F

出版信息

Br J Pharmacol. 1970 Feb;38(2):416-32. doi: 10.1111/j.1476-5381.1970.tb08529.x.

Abstract
  1. AQ 110 is a beta-adrenoceptor agonist which, like isoprenaline and salbutamol, acts directly on the receptors.2. Compared with isoprenaline, AQ 110 has relatively stronger actions on bronchial and vascular smooth muscle (beta(2)-adrenoceptors) than stimulant effects on heart muscle (beta(1)-adrenoceptors). The beta(2)-selectivity of AQ 110 is, however, much less than that of salbutamol, mainly due to the weak cardiac actions of the latter.3. At doses which were equipotent in decreasing the bronchoconstrictor effect produced by a standard dose of 5-hydroxytryptamine, AQ 110 had marginally less hypotensive action than salbutamol and considerably less than isoprenaline.4. Although AQ 110, unlike salbutamol, possesses a catechol group it was found not to be a substrate for catechol-O-methyl transferase and this is considered to account for its significantly prolonged action, compared with isoprenaline, in vivo.
摘要
  1. AQ 110是一种β-肾上腺素能受体激动剂,与异丙肾上腺素和沙丁胺醇一样,直接作用于受体。

  2. 与异丙肾上腺素相比,AQ 110对支气管和血管平滑肌(β₂-肾上腺素能受体)的作用相对强于对心肌(β₁-肾上腺素能受体)的兴奋作用。然而,AQ 110的β₂-选择性远低于沙丁胺醇,主要是因为后者的心脏作用较弱。

  3. 在降低标准剂量5-羟色胺产生的支气管收缩效应方面等效的剂量下,AQ 110的降压作用略低于沙丁胺醇,且远低于异丙肾上腺素。

  4. 虽然与沙丁胺醇不同,AQ 110含有一个儿茶酚基团,但发现它不是儿茶酚-O-甲基转移酶的底物,这被认为是其在体内作用时间比异丙肾上腺素显著延长的原因。

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