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Non-sedating antihistamines block G-protein-gated inwardly rectifying K+ channels.
I-Shan Chen
1
,
2 ,
Chang Liu
1
,
2 ,
Michihiro Tateyama
1
,
2 ,
Izhar Karbat
3 ,
Motonari Uesugi
4
,
5 ,
Eitan Reuveny
3 ,
Yoshihiro Kubo
1
,
2
September 2019
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Abstract
A second-generation antihistamine, terfenadine, is known to induce arrhythmia by blocking hERG channels. In this study, we have shown that terfenadine also inhibits the activity of G-protein-gated inwardly rectifying K+ (GIRK) channels, which regulate the excitability of neurons and cardiomyocytes. To clarify the underlying mechanism(s), we examined the effects of several antihistamines on GIRK channels and identified the structural determinant for the inhibition.