Fenfluramine blocks low-Mg2+-induced epileptiform activity in rat entorhinal cortex

Epilepsia. 2000 Aug;41(8):925-8. doi: 10.1111/j.1528-1157.2000.tb00273.x.

Abstract

Purpose: The entorhinal cortex (EC) represents the main input structure to the hippocampus and seems to be critically involved in temporal lobe epilepsy. Considering that the EC receives a strong serotonergic projection from the raphe nuclei and expresses a high density of serotonin (5-HT) receptors, the effect of the 5-HT-releasing drug fenfluramine (FFA) on epileptiform activity generated in the EC was investigated in an in vitro model of epilepsy.

Methods: The experiments were performed on 43 horizontal slices containing the EC, the subiculum, and the hippocampal formation obtained from 230-250 g adult Wistar rats. Using extracellular recording techniques, we investigated the effect of bath-applied FFA (200 micromol/L to 1 mmol/L) on epileptiform activity induced by omitting MgSO4 from the artificial cerebrospinal fluid.

Results: We demonstrate that FFA reversibly blocks epileptiform activity in the EC. Surprisingly, in the presence of the 5-HT uptake blocker paroxetine, the FFA-induced effect was diminished. Coapplication of the 5-HT1A receptor antagonist WAY100635 prevented the FFA-induced anticonvulsive effect, suggesting that (a) the FFA-induced suppression of epileptiform activity is mediated by the release of 5-HT from synaptic terminals within the EC rather than by an unspecific effect of FFA and (b) released 5-HT most likely blocks the activity by activation of 5-HT1A receptors.

Conclusion: FFA, which is primarily used because of its anorectic activity, might get an additional therapeutic value in the treatment of temporal lobe epilepsy with parahippocampal involvement.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / therapeutic use
  • Disease Models, Animal
  • Entorhinal Cortex / drug effects
  • Entorhinal Cortex / physiopathology*
  • Epilepsy / metabolism*
  • Epilepsy / physiopathology
  • Epilepsy / prevention & control*
  • Epilepsy, Temporal Lobe / drug therapy
  • Epilepsy, Temporal Lobe / physiopathology
  • Extracellular Space / metabolism
  • Fenfluramine / pharmacology*
  • Fenfluramine / therapeutic use
  • Hippocampus / drug effects
  • Hippocampus / physiopathology
  • In Vitro Techniques
  • Magnesium / administration & dosage
  • Magnesium / cerebrospinal fluid
  • Magnesium / metabolism*
  • Paroxetine / pharmacology
  • Piperazines / pharmacology
  • Presynaptic Terminals / drug effects
  • Presynaptic Terminals / metabolism
  • Pyridines / pharmacology
  • Rats
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / physiology
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Serotonin / metabolism
  • Serotonin / physiology
  • Serotonin Agents / pharmacology*
  • Serotonin Agents / therapeutic use
  • Serotonin Antagonists / pharmacology

Substances

  • Anticonvulsants
  • Piperazines
  • Pyridines
  • Receptors, Serotonin
  • Serotonin Agents
  • Serotonin Antagonists
  • Serotonin Uptake Inhibitors
  • Fenfluramine
  • Serotonin
  • Paroxetine
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide
  • Magnesium