Effects of flecainide and quinidine on Kv4.2 currents: voltage dependence and role of S6 valines

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Population

COS7 cells expressing wild-type Kv4.2 channels, N-terminal deletion, and valine mutations

Design

Preclinical

Authors

Discussion

S6 valines mediate voltage-dependent Kv4.2 block by flecainide and quinidine; leaves open translation to human electrophysiology or drug design.

Population

COS7 cells expressing wild-type Kv4.2 channels (Kv4.2WT), N-terminal deletion (N-del), and valine mutations (V[402,404]I and N-del/V[402,404]I)

Intervention

Flecainide and quinidine

Outcome

Inhibition of Kv4.2 currents and voltage dependence of blocksurrogate

S6 valines at positions 402 and 404 play an important role in mediating voltage-dependent block of Kv4.2 channels by quinidine and flecainide.

Caballero et al. (2003) studied this question.

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S6 valines mediate voltage-dependent Kv4.2 block by flecainide and quinidine; leaves open translation to human electrophysiology or drug design.