title: [Electrophysiology mechanisms of 4-butyl-alpha-agarofuran: a new anxiolytic and antidepressant drug].
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.
authors.affiliation: 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.
authors.forename: Chun-Lin
authors.initials: CL
authors.lastname: Chen
authors.forename: Wei-Ping
authors.initials: WP
authors.lastname: Wang
authors.forename: Ling
authors.initials: L
authors.lastname: Wang
authors.forename: Xiao-Liang
authors.initials: XL
authors.lastname: Wang
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000494:pharmacology*; D020746:Calcium Channels, L-Type / Q000187:drug effects*; D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000166:cytology*; D018118:Chloride Channels / Q000187:drug effects; D051668:Delayed Rectifier Potassium Channels / Q000187:drug effects; D057809:HEK293 Cells; D006801:Humans; D009474:Neurons / Q000166:cytology; D018408:Patch-Clamp Techniques; D024642:Potassium Channels, Voltage-Gated / Q000187:drug effects*; D051381:Rats; D017208:Rats, Wistar; D012717:Sesquiterpenes / Q000494:pharmacology*; D051669:Shab Potassium Channels / Q000187:drug effects; D061566:Voltage-Gated Sodium Channels / Q000187:drug effects
chemical_list: D000928:Antidepressive Agents; D020746:Calcium Channels, L-Type; D018118:Chloride Channels; D051668:Delayed Rectifier Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D012717:Sesquiterpenes; D051669:Shab Potassium Channels; D061566:Voltage-Gated Sodium Channels; C500825:alpha-agarofuran