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舒马曲坦鼻喷雾剂(英明格)对离体大鼠气管平滑肌的作用。

Effects of sumatriptan nasal spray (Imigran) on isolated rat's tracheal smooth muscle.

作者信息

Cheng Li-Hsiang, Wu Pei-Chuan, Liu Shao-Cheng, Chiu Feng-Shiang, Chu Yueng-Hsiang, Chang Ying-Nan, Wang Hsing-Won

机构信息

Department of Otolaryngology-Head and Neck Surgery, National Defense Medical Center, Tri-Service General Hospital, Taipei, Taiwan, Republic of China.

出版信息

Eur Arch Otorhinolaryngol. 2015 Oct;272(10):2861-5. doi: 10.1007/s00405-014-3392-9. Epub 2014 Nov 14.

Abstract

Sumatriptan (Imigran) is a potent and highly selective 5-HT1 receptor agonist often used in treating acute migraine. Intranasal sumatriptan is well absorbed and is generally effective in relieving headache. However, the effects of Imigran given intratracheally have rarely been well explored. We aimed to verify the effect of Imigran, which acts on the tracheal smooth muscle directly in vitro. We examined the effectiveness of Imigran on isolated rat tracheal smooth muscle by testing: (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 the addition of methacholine to the incubation medium caused the trachea to contract in a dose-dependent manner. The addition of Imigran at doses of 10(-5) M or above elicited a significant relaxation response to 10(-6) M methacholine-induced contraction. Imigran could inhibit electrical field stimulation-induced spike contraction. It also had a minimal effect on the basal tension of trachea as the concentration increased. The study indicated high concentrations of Imigran could cause bronchodilation to reduce asthma attacks not only by blocking parasympathetic tone, but also by directly antagonizing the effect of cholinergic receptors.

摘要

舒马曲坦(英明格)是一种强效且高度选择性的5-羟色胺1(5-HT1)受体激动剂,常用于治疗急性偏头痛。鼻内使用舒马曲坦吸收良好,通常能有效缓解头痛。然而,气管内给予英明格的效果鲜有深入研究。我们旨在验证英明格在体外直接作用于气管平滑肌的效果。我们通过测试以下方面来检验英明格对离体大鼠气管平滑肌的有效性:(1)对气管平滑肌静息张力的影响;(2)对作为副交感神经模拟剂的10⁻⁶ M乙酰甲胆碱引起的收缩的影响;(3)药物对电诱导的气管平滑肌收缩的影响。结果表明,向孵育培养基中添加乙酰甲胆碱会使气管以剂量依赖性方式收缩。添加10⁻⁵ M及以上剂量的英明格会引发对10⁻⁶ M乙酰甲胆碱诱导的收缩的显著舒张反应。英明格可抑制电场刺激诱导的尖峰收缩。随着浓度增加,它对气管的基础张力影响也最小。该研究表明,高浓度的英明格不仅可通过阻断副交感神经张力,还可通过直接拮抗胆碱能受体的作用来引起支气管扩张,从而减轻哮喘发作。

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