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班布特罗和特布他林对离体大鼠气管平滑肌的影响。

Effects of bambuterol and terbutaline on isolated rat's tracheal smooth muscle.

机构信息

Department of Otolaryngology-Head and Neck Surgery, Tri-Service General Hospital, National Defense Medical Center, No. 325, Sect. 2, Cheng-Gung Road, Neihu District, 114 Taipei, Taiwan, ROC.

出版信息

Eur Arch Otorhinolaryngol. 2010 Aug;267(8):1305-11. doi: 10.1007/s00405-009-1173-7. Epub 2009 Dec 12.

Abstract

Terbutaline (Bricanyl) and its prodrug Bambuterol (Bambec) are highly potent beta(2)-adrenoceptor agonists often used in asthma patients. Terbutaline in the form of inhaled short-acting bronchodilator relieves asthmatic symptoms. However, the effects of bambuterol given intratracheally have rarely been explored. To verify the effect of bambuterol and terbutaline, which act on the tracheal smooth muscle directly in vitro, we used our preparation to test the effects of bambuterol on isolated rat's tracheal smooth muscle compared with terbutaline. The following assessments of bambuterol and terbutaline were performed: (1) effect on tracheal smooth muscle resting tension; (2) effect on contraction caused by 10(-6) M methacholine as a parasympathetic mimetic; (3) effect of the drugs on electrically induced tracheal smooth muscle contractions. The results indicated that adding bambuterol induced a significant further contraction to 10(-6) M methacholine-induced contraction when the preparation was increased to 10(-4) M. But terbutaline elicited a relaxation response at a dose of 10(-6) M or more. Both bambuterol and terbutaline could inhibit electrical field stimulation (EFS) induced spike contraction. Terbutaline had an anti-cholinergic effect that could relieve asthmatic symptoms. But the effect of bambuterol acting on tracheal smooth muscle directly was controversial.

摘要

特布他林(博利康尼)及其前体药物班布特罗(班比特罗)是强效的β2-肾上腺素受体激动剂,常用于哮喘患者。特布他林作为吸入性短效支气管扩张剂可缓解哮喘症状。然而,班布特罗经气管内给药的作用很少被探讨。为了验证直接作用于气管平滑肌的班布特罗和特布他林的作用,我们使用我们的制剂来测试班布特罗对分离的大鼠气管平滑肌的作用,并与特布他林进行比较。对班布特罗和特布他林进行了以下评估:(1)对气管平滑肌静息张力的影响;(2)对 10(-6)M 乙酰甲胆碱引起的收缩的影响,作为副交感神经拟似物;(3)药物对电诱导的气管平滑肌收缩的影响。结果表明,当制剂增加到 10(-4)M 时,加入班布特罗会引起对 10(-6)M 乙酰甲胆碱诱导收缩的显著进一步收缩。但特布他林在 10(-6)M 或更高剂量时会引起松弛反应。班布特罗和特布他林均可抑制电刺激(EFS)诱导的峰收缩。特布他林具有抗胆碱能作用,可缓解哮喘症状。但是,班布特罗直接作用于气管平滑肌的作用存在争议。

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