Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Molecules ; 28(13)2023 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-37446837

RESUMO

Erythromycin is one of the few compounds that remarkably increase ether-a-go-go-related gene (hERG) inhibition from room temperature (RT) to physiological temperature (PT). Understanding how erythromycin inhibits the hERG could help us to decide which compounds are needed for further studies. The whole-cell patch clamp technique was used to investigate the effects of erythromycin on hERG channels at different temperatures. While erythromycin caused a concentration-dependent inhibition of cardiac hERG channels, it also shifted the steady-state activation and steady-state inactivation of the channel to the left and significantly accelerated the onset of inactivation at both temperatures, although temperature itself caused a profound change in the dynamics of hERG channels. Our data also suggest that the binding pattern to S6 of the channels changes at PT. In contrast, cisapride, a well-known hERG blocker whose inhibition is not affected by temperature, does not change its critical binding sites after the temperature is raised to PT. Our data suggest that erythromycin is unique and that the shift in hERG inhibition may not apply to other compounds.


Assuntos
Eritromicina , Canais de Potássio Éter-A-Go-Go , Eritromicina/farmacologia , Temperatura , Cisaprida/metabolismo , Cisaprida/farmacologia , Coração , Canal de Potássio ERG1 , Bloqueadores dos Canais de Potássio/farmacologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...