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Eur Biophys J ; 46(6): 517-523, 2017 Sep.
Article in English | MEDLINE | ID: mdl-28108814

ABSTRACT

Apamin is frequently used as a specific blocker of small-conductance Ca2+-activated (SK type) K+ channels. Here we show that the small neurotoxin is not as specific as anticipated. It is also a high-affinity inhibitor with an IC50 of 13 nM of the Kv1.3 channel; it blocks the latter with potency similar to the Kv1.3 blocker PAP-1. Since SK type channels and Kv1.3 channels are frequently coexpressed in different tissues such as cells of the immune system, apamin must be used with caution as a pharmacological tool.


Subject(s)
Apamin/toxicity , Kv1.3 Potassium Channel/antagonists & inhibitors , Neurotoxins/toxicity , Potassium Channel Blockers/toxicity , Potassium Channels, Calcium-Activated/antagonists & inhibitors , Electrophysiological Phenomena/drug effects , HEK293 Cells , Humans , Inhibitory Concentration 50 , Kv1.3 Potassium Channel/metabolism , Pancreatitis-Associated Proteins , Potassium Channels, Calcium-Activated/metabolism
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