Quinidine normalizes the open duration of slow‐channel mutants of the acetylcholine receptor
作者:
Takayasu Fukudome,
Kinji Ohno,
Joan Brengman,
Andrew Engel,
期刊:
NeuroReport
(OVID Available online 1998)
卷期:
Volume 9,
issue 8
页码: 1907-1911
ISSN:0959-4965
年代: 1998
出版商: OVID
关键词: Acetylcholine receptor;Channel block;Patch-clamp;Quinidine;Slow channel congenital myasthenic syndrome
数据来源: OVID
摘要:
QUINIDINE is a long-lived open-channel blocker of the wild-type endplate acetylcholine receptor (AChR). To test the hypothesis that quinidine can normalize the prolonged channel opening events of slow-channel mutants of human AChR, we expressed wild-type AChR and five well characterized slow-channel mutants of AChR in HEK 293 cells and monitored the effects of quinidine on acetylcholine-induced channel currents. Quinidine shortens the longest component of channel opening burst (τ3b) of both wild-type and mutant AChRs in a concentration-dependent manner, and 5 μM quini-dine reduces τ3bof the mutant AChRs to that of wild-type AChRs in the absence of quinidine. Because this concentration of quinidine is attainable in clinical practice, the findings predict a therapeutic effect for quinidine in the slow-channel congenital myasthenic syndrome.
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