Clofilium inhibits Slick and Slack potassium channels
Maria de los Angeles Tejada,1 Kathleen Stolpe,1 Anne-Kristine Meinild,2 Dan A Klaerke11Department of Physiology and Biochemistry, Faculty of Life Sciences, 2Institute of Biology, Faculty of Science, University of Copenhagen, Copenhagen, DenmarkAbstract: Slick and Slack high-conductance potassium cha...
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Dove Medical Press
2012
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oai:doaj.org-article:cb3eaff9a78d4b9caa893057de1af6742021-12-02T00:25:57ZClofilium inhibits Slick and Slack potassium channels1177-54751177-5491https://doaj.org/article/cb3eaff9a78d4b9caa893057de1af6742012-12-01T00:00:00Zhttp://www.dovepress.com/clofilium-inhibits-slick-and-slack-potassium-channels-a11748https://doaj.org/toc/1177-5475https://doaj.org/toc/1177-5491Maria de los Angeles Tejada,1 Kathleen Stolpe,1 Anne-Kristine Meinild,2 Dan A Klaerke11Department of Physiology and Biochemistry, Faculty of Life Sciences, 2Institute of Biology, Faculty of Science, University of Copenhagen, Copenhagen, DenmarkAbstract: Slick and Slack high-conductance potassium channels have been recently discovered, and are found in the central nervous system and in the heart. Both channels are activated by Na+ and Cl-, and Slick channels are also inhibited by adenosine triphospate (ATP). An important role of setting the resting membrane potential and controlling the basal excitability of neurons has been suggested for these channels. In addition, no specific blockers for these channels are known up to the present. With the purpose of studying the pharmacological characteristics of Slick and Slack channels, the effects of exposure to the antiarrhythmic compound clofilium were evaluated. Clofilium was able to modulate the activity of Slick and Slack channels effectively, with a stronger effect on Slack than Slick channels. In order to evaluate the pharmacological behavior of Slick and Slack channels further, 38 commonly used potassium channel blockers were tested. Screening of these compounds did not reveal any modulators of Slick and Slack channels, except for clofilium. The present study provides a first approach towards elucidating the pharmacological characteristics of Slick and Slack channels and could be the basis for future studies aimed at developing potent and specific blockers and activators for these channels.Keywords: Slo2.1, Slo2.2, clofilium, potassium channel blockersTejada MAStolpe KMeinild AKKlaerke DADove Medical PressarticleMedicine (General)R5-920ENBiologics: Targets & Therapy, Vol 2012, Iss default, Pp 465-470 (2012) |
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Medicine (General) R5-920 Tejada MA Stolpe K Meinild AK Klaerke DA Clofilium inhibits Slick and Slack potassium channels |
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Maria de los Angeles Tejada,1 Kathleen Stolpe,1 Anne-Kristine Meinild,2 Dan A Klaerke11Department of Physiology and Biochemistry, Faculty of Life Sciences, 2Institute of Biology, Faculty of Science, University of Copenhagen, Copenhagen, DenmarkAbstract: Slick and Slack high-conductance potassium channels have been recently discovered, and are found in the central nervous system and in the heart. Both channels are activated by Na+ and Cl-, and Slick channels are also inhibited by adenosine triphospate (ATP). An important role of setting the resting membrane potential and controlling the basal excitability of neurons has been suggested for these channels. In addition, no specific blockers for these channels are known up to the present. With the purpose of studying the pharmacological characteristics of Slick and Slack channels, the effects of exposure to the antiarrhythmic compound clofilium were evaluated. Clofilium was able to modulate the activity of Slick and Slack channels effectively, with a stronger effect on Slack than Slick channels. In order to evaluate the pharmacological behavior of Slick and Slack channels further, 38 commonly used potassium channel blockers were tested. Screening of these compounds did not reveal any modulators of Slick and Slack channels, except for clofilium. The present study provides a first approach towards elucidating the pharmacological characteristics of Slick and Slack channels and could be the basis for future studies aimed at developing potent and specific blockers and activators for these channels.Keywords: Slo2.1, Slo2.2, clofilium, potassium channel blockers |
format |
article |
author |
Tejada MA Stolpe K Meinild AK Klaerke DA |
author_facet |
Tejada MA Stolpe K Meinild AK Klaerke DA |
author_sort |
Tejada MA |
title |
Clofilium inhibits Slick and Slack potassium channels |
title_short |
Clofilium inhibits Slick and Slack potassium channels |
title_full |
Clofilium inhibits Slick and Slack potassium channels |
title_fullStr |
Clofilium inhibits Slick and Slack potassium channels |
title_full_unstemmed |
Clofilium inhibits Slick and Slack potassium channels |
title_sort |
clofilium inhibits slick and slack potassium channels |
publisher |
Dove Medical Press |
publishDate |
2012 |
url |
https://doaj.org/article/cb3eaff9a78d4b9caa893057de1af674 |
work_keys_str_mv |
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1718403767240491008 |