硫代乙酰胆碱
化学
氨基甲酸酯
基质(水族馆)
药理学
前药
乙酰胆碱酯酶
效力
胆碱酯酶
酶
立体化学
生物化学
特布他林
阿切
生物
体外
免疫学
生态学
哮喘
作者
Anders Tunek,Leif‐Åke Svensson
出处
期刊:PubMed
日期:1988-09-01
卷期号:16 (5): 759-64
被引量:25
摘要
Bambuterol, the bis-dimethyl carbamate prodrug of terbutaline, was tested for its potency in inhibiting cholinesterases in human blood. Preincubation of blood with bambuterol in the absence of thiocholine ester substrate was essential for obtaining maximal inhibition. The inhibition exerted by bambuterol after such preincubation was reversible and noncompetitive. Bambuterol was an extremely effective inhibitor of cholinesterase when butyrylthiocholine was used as substrate (I50 = 1.7 +/- 0.3 x 10(-8) M, N = 10) whereas it was 2400-fold less efficient in inhibiting cholinesterase with acetylthiocholine as substrate (I50 = 4.1 +/- 0.5 x 10(-5) M, N = 10). Because butyrylthiocholine is the preferred substrate for cholinesterase (EC 3.1.1.8) and acetylthiocholine for acetylcholinesterase (EC 3.1.1.7), these results indicate that bambuterol is a remarkably selective and potent inhibitor of cholinesterase.
科研通智能强力驱动
Strongly Powered by AbleSci AI