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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Autores principales: Tejada MA, Stolpe K, Meinild AK, Klaerke DA
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Publicado: Dove Medical Press 2012
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spelling 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)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Tejada MA
Stolpe K
Meinild AK
Klaerke DA
Clofilium inhibits Slick and Slack potassium channels
description 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 AT tejadama clofiliuminhibitsslickandslackpotassiumchannels
AT stolpek clofiliuminhibitsslickandslackpotassiumchannels
AT meinildak clofiliuminhibitsslickandslackpotassiumchannels
AT klaerkeda clofiliuminhibitsslickandslackpotassiumchannels
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