氮卓斯汀和去甲基氮卓斯汀可抑制人气道平滑肌中乙酰胆碱诱导的收缩和去极化。

Azelastine and desmethylazelastine suppress acetylcholine-induced contraction and depolarization in human airway smooth muscle.

作者信息

Richards I S, Miller L, Solomon D, Kulkarni A, Brooks S, Sperelakis N

机构信息

Department of Environmental and Occupational Health, College of Public Health, University of South Florida, Tampa 33612.

出版信息

Eur J Pharmacol. 1990 Sep 21;186(2-3):331-4. doi: 10.1016/0014-2999(90)90455-f.

DOI:10.1016/0014-2999(90)90455-f

PMID:1981189

Abstract

We examined the effects of a new anti-asthmatic drug, azelastine, and its principal metabolite, desmethylazelastine, on the in vitro electromechanical response of human airway smooth muscle during cholinergic stimulation. Membrane potential and isometric force were simultaneously measured using an intracellular microelectrode and a microforce transducer. Desmethylazelastine significantly suppressed acetylcholine-induced depolarization and contraction at 10(-6) M, whereas azelastine produced similar results at 10(-4) M, suggesting that the metabolite may be the principal compound acting upon the airway smooth muscle cell.

摘要

我们研究了一种新型抗哮喘药物氮卓斯汀及其主要代谢产物去甲基氮卓斯汀对胆碱能刺激期间人气道平滑肌体外机电反应的影响。使用细胞内微电极和微力传感器同时测量膜电位和等长力。去甲基氮卓斯汀在10^(-6) M时可显著抑制乙酰胆碱诱导的去极化和收缩，而氮卓斯汀在10^(-4) M时产生类似结果，这表明该代谢产物可能是作用于气道平滑肌细胞的主要化合物。