Electrophysiology mechanisms of 4-butyl-alpha-agarofuran: a new anxiolytic and antidepressant drug / 药学学报
Acta Pharmaceutica Sinica
; (12): 38-44, 2013.
Article
en Zh
| WPRIM
| ID: wpr-274593
Biblioteca responsable:
WPRO
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:
1
Base de datos:
WPRIM
Asunto principal:
Farmacología
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Sesquiterpenos
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Células Cultivadas
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Corteza Cerebral
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Ratas Wistar
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Canales de Cloruro
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Técnicas de Placa-Clamp
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Canales de Calcio Tipo L
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Biología Celular
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Canales de Potasio con Entrada de Voltaje
Límite:
Animals
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Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2013
Tipo del documento:
Article