The GABA(A) receptor complex
as a target for fluoxetine action

by
Tunnicliff G, Schindler NL, Crites GJ,
Goldenberg R, Yochum A, Malatynska E
Department of Biochemistry,
Indiana University School of Medicine,
Evansville 47712, USA.
gtunnic@iupui.edu
Neurochem Res 1999 Oct; 24(10):1271-6


ABSTRACT

The clinically important antidepressant fluoxetine is established as a selective serotonin reuptake inhibitor. This study demonstrates that fluoxetine also interacts with the GABA(A) receptor complex. At concentrations above 10 microM fluoxetine inhibited the binding of both [3H]GABA (IC50 = 2 mM) and [3H]flunitrazepam (IC50 = 132 microM) to the GABA(A) receptor complex in brain cortical membranes. Low fluoxetine concentrations (1 nM) enhanced GABA-stimulated Cl- uptake by a rat cerebral cortical vesicular preparation. At higher concentrations (100 microM and 1 mM), however, fluoxetine inhibited GABA-stimulated Cl- uptake, an effect related to a reduction in Emax. These observations might assist in an explanation of the basis of the antidepressant action of fluoxetine.
GABA
SSRIs
RIMAs
Anxiety
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Selegiline
Fluoxetine
GABA and sleep
MAO-B inhibition
Fluoxetine and GABA(A)
Tryptophan plus fluoxetine
Antidepressant mechanisms
Comparisons and metabolites
Fluoxetine (Prozac) and 5-HT2c
GABA, pain and the cerebral cortex
GABAergic dysfunction in mood disorders
How effective are commonly prescribed antidepressants?


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