Electrophysiology mechanisms of 4-butyl-alpha-agarofuran: a new anxiolytic and antidepressant drug.
- Author:
Chun-Lin CHEN
1
;
Wei-Ping WANG
;
Ling WANG
;
Xiao-Liang WANG
Author Information
1. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antidepressive Agents;
pharmacology;
Calcium Channels, L-Type;
drug effects;
Cells, Cultured;
Cerebral Cortex;
cytology;
Chloride Channels;
drug effects;
Delayed Rectifier Potassium Channels;
drug effects;
HEK293 Cells;
Humans;
Neurons;
cytology;
Patch-Clamp Techniques;
Potassium Channels, Voltage-Gated;
drug effects;
Rats;
Rats, Wistar;
Sesquiterpenes;
pharmacology;
Shab Potassium Channels;
drug effects;
Voltage-Gated Sodium Channels;
drug effects
- From:
Acta Pharmaceutica Sinica
2013;48(1):38-44
- CountryChina
- Language:Chinese
-
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.
