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Comparison of the bronchodilator and cardiovascular actions of salbutamol, isoprenaline and orciprenaline in guinea-pigs and dogs.沙丁胺醇、异丙肾上腺素和奥西那林对豚鼠和犬支气管扩张及心血管作用的比较
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Br J Pharmacol. 1974 Nov;52(3):407-17. doi: 10.1111/j.1476-5381.1974.tb08610.x.
3
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Cardiovascular effects of morphine, pethidine, diamorphine and nalorphine on the cat and rabbit.吗啡、哌替啶、二醋吗啡和烯丙吗啡对猫和兔的心血管作用。
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Naunyn Schmiedebergs Arch Pharmacol. 1975;287(2):227-32. doi: 10.1007/BF00510454.

本文引用的文献

1
THE PHARMACOLOGY OF ISOLATED VEINS.离体静脉的药理学
Br J Pharmacol Chemother. 1965 Jun;24(3):742-51. doi: 10.1111/j.1476-5381.1965.tb01630.x.
2
A COMPARISON OF THE CARDIAC STIMULATING AND BRONCHODILATOR ACTIONS OF SELECTED SYMPATHOMIMETIC AMINES.某些拟交感神经胺的心脏刺激作用与支气管扩张作用的比较
Proc Soc Exp Biol Med. 1964 Jun;116:331-3. doi: 10.3181/00379727-116-29239.
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The relation between chemical structure and biological activity. Discussion of possibilities, pitfalls and limitations.
J Pharm Pharmacol. 1963 May;15:285-316. doi: 10.1111/j.2042-7158.1963.tb12787.x.
4
Differentiation of receptor systems activated by sympathomimetic amines.拟交感胺激活的受体系统的分化
Nature. 1967 May 6;214(5088):597-8. doi: 10.1038/214597a0.
5
Salbutamol: a new, selective beta-adrenoceptive receptor stimulant.沙丁胺醇:一种新型的选择性β-肾上腺素能受体兴奋剂。
Br J Pharmacol. 1969 Jan;35(1):141-51. doi: 10.1111/j.1476-5381.1969.tb07975.x.
6
Pharmacologic potency and selectivity of a new bronchodilator agent: soterenol (MJ 1992).一种新型支气管扩张剂的药理效力和选择性:索特仑(MJ 1992)。
J Pharmacol Exp Ther. 1968 Dec;164(2):290-301.
7
Studies on tetradhydroisoquinolines (THI). II. Pharmacological action on the cardiovascular system.四氢异喹啉类化合物(THI)的研究。II. 对心血管系统的药理作用。
Jpn J Pharmacol. 1967 Jun;17(2):153-63. doi: 10.1254/jjp.17.153.
8
Studies on tetrahydroisoquinolines (THI). I. Bronchodilator activity and structure-activity relationship.四氢异喹啉(THI)的研究。I. 支气管扩张活性及构效关系。
Jpn J Pharmacol. 1967 Jun;17(2):143-52. doi: 10.1254/jjp.17.143.
9
A simple isolated nerve-blood vessel preparation.一种简单的离体神经-血管标本。
Aust J Exp Biol Med Sci. 1965 Oct;43(5):639-56. doi: 10.1038/icb.1965.48.
10
Catechol-o-methyl transferase inhibition and potentiation of epinephrine responses by desmethylpapavernine.儿茶酚 - O - 甲基转移酶抑制作用以及去甲基罂粟碱对肾上腺素反应的增强作用。
Biochem Pharmacol. 1965 May;14(5):823-9. doi: 10.1016/0006-2952(65)90101-2.

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.

DOI:10.1111/j.1476-5381.1970.tb08529.x
PMID:4392103
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1702809/
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。