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December 1, 1997British Journal of Pharmacology

Effect of fluoxetine on a neuronal, voltage‐dependent potassium channel (Kv1.1)

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Key result

Fluoxetine caused a use- and dose-dependent blockade of the neuronal voltage-dependent potassium channel Kv1.1, slowing both activation and deactivation kinetics.

Population

Xenopus laevis oocytes expressing a neuronal, voltage-dependent potassium (K+) channel (RCK1; Kv1.1)

Design

Preclinical

Authors

JTJan TytgatMadrid Institute for Advanced StudiesCMC. MaertensUniversitair Ziekenhuis LeuvenPDPaul DaenensUniversitair Ziekenhuis Leuven

Discussion

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Overview

Should not change fluoxetine prescribing; leaves open whether Kv1.1 blockade contributes to clinical adverse effects.

Structured PICO

P
Population
Xenopus laevis oocytes expressing a neuronal, voltage-dependent potassium (K+) channel (RCK1; Kv1.1)
I
Intervention
Fluoxetine
O
Outcome
Blockade of K+ currents and effects on activation and deactivation kineticssurrogate

Fluoxetine blocks the neuronal voltage-dependent potassium channel Kv1.1 in a use- and dose-dependent manner, providing a biophysical model that may help explain clinical symptoms seen with elevated serum concentrations.

Limitations

  • The channel is not very potently blocked by fluoxetine when expressed in oocytes.

Cite This Study

Tytgat et al. (1997) studied this question. Fluoxetine was evaluated on Blockade of K+ currents and channel kinetics. Fluoxetine caused a use- and dose-dependent blockade of the neuronal voltage-dependent potassium channel Kv1.1, slowing both activation and deactivation kinetics.

synapsesocial.com/papers/6a9fd60bdd8cd84ce6d558eehttps://doi.org/10.1038/sj.bjp.0701545
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Also Consider

Synapse has enriched 2 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Use-dependent block and use-dependent unblock of the delayed rectifier K+ current by almokalant in rabbit ventricular myocytes.1993 · 137 citations
  2. 2Immunohistochemical Localization of Five Members of the KV1 Channel Subunits: Contrasting Subcellular Locations and Neuron‐specific Co‐localizations in Rat Brain1995 · 329 citations