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From the Department of Physiology and Biophysics, The University of Iowa, Iowa City, Iowa 52242
Dihydropyridines (DHPs) are well known for their effects on L-type voltage-dependent Ca2+ channels. However, these drugs also affect other voltage-dependent ion channels, including Shaker K+ channels. We examined the effects of DHPs on the Shaker K+ channels expressed in Xenopus oocytes. Intracellular applications of
DHPs quickly and reversibly induced apparent inactivation in the Shaker K+ mutant channels with disrupted
N- and C-type inactivation. We found that DHPs interact with the open state of the channel as evidenced by the
decreased mean open time. The DHPs effects are voltage-dependent, becoming more effective with hyperpolarization. A model which involves binding of two DHP molecules to the channel is consistent with the results obtained in our experiments.
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