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沙丁胺醇:一种新型的选择性β-肾上腺素能受体兴奋剂。

Salbutamol: a new, selective beta-adrenoceptive receptor stimulant.

作者信息

Cullum V A, Farmer J B, Jack D, Levy G P

出版信息

Br J Pharmacol. 1969 Jan;35(1):141-51. doi: 10.1111/j.1476-5381.1969.tb07975.x.

DOI:10.1111/j.1476-5381.1969.tb07975.x
PMID:5762037
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1703073/
Abstract
  1. Salbutamol is a beta-adrenoceptive receptor stimulant. Its pharmacological actions are reduced or abolished by beta-receptor antagonists.2. In anaesthetized animals, salbutamol, given intravenously, was slightly less active than isoprenaline in preventing spasm of bronchial smooth muscle but was considerably less active as a cardiac stimulant and vasodepressor substance. Its duration of action was about 2 to 3 times that of isoprenaline.3. Salbutamol given by mouth or aerosol to conscious guinea-pigs, greatly diminished bronchospasm caused by inhalation of acetylcholine. By mouth, salbutamol was more active and had a longer duration than isoprenaline or orciprenaline without affecting heart rate. By aerosol, salbutamol was approximately 10 times as active as isoprenaline and 100 times as active as orciprenaline. Its duration of action was much longer than that of isoprenaline or orciprenaline. Only isoprenaline produced an increase in heart rate by the aerosol route.4. On isolated guinea-pig trachea salbutamol had about 1/10 the activity of isoprenaline, on isolated atria about 1/2000.
摘要
  1. 沙丁胺醇是一种β-肾上腺素能受体兴奋剂。其药理作用可被β-受体拮抗剂减弱或消除。

  2. 在麻醉动物中,静脉注射沙丁胺醇在预防支气管平滑肌痉挛方面的活性略低于异丙肾上腺素,但作为心脏兴奋剂和血管减压物质的活性则低得多。其作用持续时间约为异丙肾上腺素的2至3倍。

  3. 给清醒的豚鼠口服或雾化吸入沙丁胺醇,可大大减轻因吸入乙酰胆碱引起的支气管痉挛。口服时,沙丁胺醇比异丙肾上腺素或奥西那林更有效,作用持续时间更长,且不影响心率。通过雾化吸入,沙丁胺醇的活性约为异丙肾上腺素的10倍,奥西那林的100倍。其作用持续时间比异丙肾上腺素或奥西那林长得多。只有异丙肾上腺素通过雾化吸入途径会使心率增加。

  4. 在离体豚鼠气管上,沙丁胺醇的活性约为异丙肾上腺素的1/10,在离体心房上约为1/2000。

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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.
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Comparison of the effects of isoprenaline, orciprenaline, salbutamol and isoetharine on the cardiovascular system of anaesthetized dogs.异丙肾上腺素、奥西那林、沙丁胺醇和异他林对麻醉犬心血管系统作用的比较。
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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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