Article
Kv1.4 channel block by quinidine: evidence for a drug-induced allosteric effect.
The Journal of physiology - 15 Jan 2003
Wang Shimin, Morales Michael J, Qu Yu-Jie, Bett Glenna C L, Strauss Harold C, Rasmusson Randall L
Abstract excerpt
We studied quinidine block of Kv1.4DeltaN, a K(+) channel lacking N-type inactivation, expressed in Xenopus ooctyes. Initially, quinidine intracellularly blocked the open channel so rapidly it overlapped with activation. This rapid open channel block was reduced (non-additively) by interventions that slow C-type inactivation: [K(+)](o) elevation and an extracellular lysine to tyrosine mutation (K532Y). These...
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