Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole.
FEBS Lett
; 385(1-2): 77-80, 1996 Apr 29.
Article
en En
| MEDLINE
| ID: mdl-8641472
ABSTRACT
The widely used histamine receptor antagonists terfenadine and astemizole were shown to prolong the QT interval in electrocardiographic recordings in cases of overdose or inappropriate co-medications, indicating a possible interaction with cardiac K+ channels. Here, terfenadine and astemizole both inhibited the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fashion. In contrast, inhibition of other delayed rectifier (Kv1.1 and IsK) or inward rectifier K+ channels (IRK1) was much weaker and occurred only at high micromolar concentrations. These results suggest that blockade of HERG channels by terfenadine and astemizole might contribute to the cardiac side effects of these compounds.
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Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Canales de Potasio
/
Transactivadores
/
Terfenadina
/
Astemizol
/
Canales de Potasio con Entrada de Voltaje
/
Proteínas de Transporte de Catión
/
Proteínas de Unión al ADN
/
Antagonistas de los Receptores Histamínicos H1
Límite:
Animals
/
Humans
Idioma:
En
Revista:
FEBS Lett
Año:
1996
Tipo del documento:
Article
País de afiliación:
Alemania