Electrophysiology mechanisms of 4-butyl-alpha-agarofuran: a new anxiolytic and antidepressant drug / 药学学报
Acta Pharmaceutica Sinica
;
(12): 38-44, 2013.
Artigo
em Chinês
| WPRIM
| ID: wpr-274593
ABSTRACT
To investigate the electrophysiology mechanisms of new anxiolytic and antidepressant drug 4-butyl-alpha-agarofuran (AF-5), patch clamp-recording was used to test the effects of AF-5 on voltage-dependent sodium currents, voltage-dependent potassium currents, L-type voltage-dependent calcium currents and GABA dependent Cl(-) currents in primary cultured rat cortical neurons. Effects of AF-5 on Kv2.1 currents, expressed stably in HEK293 cells, were also tested. Our results showed that, delayed rectifier potassium currents (I(K(DR, L-type voltage-dependent calcium currents (I(LC-ca)) in primary cultured rat cortical neurons and Kv2.1 currents in HEK293 cells were significantly inhibited by AF-5, with IC50 as 6.17, 4.4 and 5.29 micromol x L(-1) respectively. However, voltage-dependent sodium currents (I(Na)), GABA dependent Cl(-) currents and transient outward potassium currents (I(K(A)) in primary cultured rat cortical neurons were not significantly blocked by AF-5. Our results concluded that, blocked I(K(DR)) and I(L-Ca) currents may be one of the mechanisms of anxiolytic and antidepression actions of AF-5.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Farmacologia
/
Sesquiterpenos
/
Células Cultivadas
/
Córtex Cerebral
/
Ratos Wistar
/
Canais de Cloreto
/
Técnicas de Patch-Clamp
/
Canais de Cálcio Tipo L
/
Biologia Celular
/
Canais de Potássio de Abertura Dependente da Tensão da Membrana
Limite:
Animais
/
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2013
Tipo de documento:
Artigo
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