| Literature DB >> 12850554 |
Georg C Terstappen1, Annalisa Pellacani, Laura Aldegheri, Francesca Graziani, Corrado Carignani, Giordano Pula, Caterina Virginio.
Abstract
The effects of fluoxetine (Prozac) on the activity of human small-conductance calcium-activated potassium (SK) channels were investigated utilizing a functional fluorescence assay with bis-(1,3-dibutylbarbituric acid)trimethine oxonol (DiBAC(4)(3)). Fluoxetine blocked SK channels stably expressed in HEK 293 cells in a concentration-dependent manner displaying half-maximal inhibitory concentrations (IC(50)) of 9 microM for hSK1, 7 microM for hSK2 and 20 microM for hSK3. The block of hSK3 channels was confirmed by whole cell patch-clamp recordings of the recombinant cells and human TE 671 cells. Fluoxetine also inhibited [(125)I]apamin binding in a concentration-dependent manner displaying IC(50) values of 63 microM for hSK1, 148 microM for hSK2 and 295 microM for hSK3. These results provide new information concerning the mechanism of therapeutic and/or side effects of one of the most widely used antidepressant drugs.Entities:
Mesh：
Substances：
Year: 2003 PMID： 12850554 DOI： 10.1016/s0304-3940(03)00574-3
Source DB: PubMed Journal: Neurosci Lett ISSN： 0304-3940 Impact factor: 3.046