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Dihydropyridine Action on Voltage-dependent Potassium Channels Expressed in Xenopus Oocytes

Dihydropyridines (DHPs) are well known for their effects on L-type voltage-dependent Ca(2+) 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. Intra...

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Detalles Bibliográficos
Autores principales: Avdonin, Vladimir, Shibata, Erwin F., Hoshi, Toshinori
Formato: Texto
Lenguaje:English
Publicado: The Rockefeller University Press 1997
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2220064/
https://www.ncbi.nlm.nih.gov/pubmed/9041446
Descripción
Sumario:Dihydropyridines (DHPs) are well known for their effects on L-type voltage-dependent Ca(2+) 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.