The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3

Reference:

Terstappen, G., Pellacani, A., Aldegheri, L., Graziani, F., Carignani, C., Pula, G. and Virginio, C., 2003. The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3. Neuroscience Letters, 346 (1-2), pp. 85-88.

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Official URL:

http://dx.doi.org/10.1016/S0304-3940(03)00574-3

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 (DiBAC4(3)). Fluoxetine blocked SK channels stably expressed in HEK 293 cells in a concentration-dependent manner displaying half-maximal inhibitory concentrations (IC50) of 9 μM for hSK1, 7 μM for hSK2 and 20 μM 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 [125I]apamin binding in a concentration-dependent manner displaying IC50 values of 63 μM for hSK1, 148 μM for hSK2 and 295 μM 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.

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