The small neurotoxin apamin blocks not only small conductance Ca2+ activated K+ channels (SK type) but also the voltage dependent Kv1.3 channel.
Eur Biophys J
; 46(6): 517-523, 2017 Sep.
Article
em En
| 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.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Apamina
/
Canais de Potássio Cálcio-Ativados
/
Bloqueadores dos Canais de Potássio
/
Canal de Potássio Kv1.3
/
Neurotoxinas
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article