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Bicuculline free base blocks voltage-activated K+ currents in rat medial preoptic neurons.
Umeå University, Faculty of Medicine, Integrative Medical Biology, Physiology.
Umeå University, Faculty of Medicine, Integrative Medical Biology, Physiology.
Umeå University, Faculty of Medicine, Integrative Medical Biology, Physiology.
2004 (English)In: Neuropharmacology, ISSN 0028-3908, Vol. 46, no 2, 285-95 p.Article in journal (Refereed) Published
Abstract [en]

The effects of the well-known GABA(A)-receptor blocker bicuculline on voltage-gated K(+) currents were studied in neurons from the medial preoptic nucleus (MPN) of rat. Whole-cell currents were recorded using the perforated-patch technique. Voltage steps from -54 to +6 mV resulted in tetraethylammonium-sensitive K(+) currents of delayed rectifier type. The total K(+) current (at 300 ms), including Ca(2+)-dependent and Ca(2+)-independent components, was reversibly reduced (17 +/- 4%) by 100 microM bicuculline methiodide and (37 +/- 5%) by 100 microM bicuculline as free base. The Ca(2+)-independent fraction (77 +/- 2%) of K(+) current evoked by a voltage step was, however, reduced (54 +/- 6%) only by bicuculline free base, but was not affected by bicuculline methiodide. The half-saturating concentration of bicuculline free base for blocking this purely voltage-gated K(+) current was 113 microM, whereas for blocking a steady Ca(2+)-dependent K(+) current it was 36 microM. The bicuculline-sensitive voltage-gated K(+) current was composed of 4-AP-sensitive and 4-AP-resistant components with different kinetic properties. No component of the purely voltage-gated K(+) current was affected neither by 100 nM alpha-dendrotoxin nor by 100 nM I-dendrotoxin. The possible K(+)-channel subtypes mediating the bicuculline-sensitive current in MPN neurons are discussed.

Place, publisher, year, edition, pages
2004. Vol. 46, no 2, 285-95 p.
Keyword [en]
Animals, Bicuculline/chemistry/*pharmacology, Cells; Cultured, Dose-Response Relationship; Drug, Male, Membrane Potentials/drug effects/physiology, Neurons/*drug effects/physiology, Potassium Channel Blockers/chemistry/*pharmacology, Potassium Channels; Voltage-Gated/*antagonists & inhibitors/physiology, Preoptic Area/*drug effects/physiology, Rats, Rats; Sprague-Dawley
Identifiers
URN: urn:nbn:se:umu:diva-12598PubMedID: 14680766OAI: oai:DiVA.org:umu-12598DiVA: diva2:152269
Available from: 2008-01-09 Created: 2008-01-09 Last updated: 2011-01-12Bibliographically approved

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