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Non‐sedating antihistamines block G‐protein‐gated inwardly rectifying K+ channels

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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+… Click to show full 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.

Keywords: protein gated; sedating antihistamines; gated inwardly; inwardly rectifying; non sedating

Journal Title: British Journal of Pharmacology
Year Published: 2019

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