The small neurotoxin apamin blocks not only small conductance Ca2+ activated K+ channels (SK type) but also the voltage dependent Kv1.3 channel

Voos Patrick; Yazar Mehtap; Lautenschlaeger Rene; Rauh Oliver; Moroni Anna; Thiel Gerhard<sup>*</sup>

doi:10.1007/s00249-016-1196-0

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The small neurotoxin apamin blocks not only small conductance Ca2+ activated K+ channels (SK type) but also the voltage dependent Kv1.3 channel

作者：Voos Patrick; Yazar Mehtap; Lautenschlaeger Rene; Rauh Oliver; Moroni Anna; Thiel Gerhard^*

来源：European Biophysics Journal, 2017, 46(6): 517-523.

DOI：10.1007/s00249-016-1196-0

摘要

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.