Electrophysiological effects of fluoxetine and duloxetine in the dorsal raphe nucleus and hippocampus

Eur J Pharmacol. 1997 Mar 26;323(1):69-73. doi: 10.1016/s0014-2999(97)00024-1.

Abstract

The cellular electrophysiological effects of duloxetine (LY248686), a dual serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine reuptake inhibitor, and the selective serotonin reuptake inhibitor fluoxetine were compared on spontaneously active neurons in the dorsal raphe nucleus and the hippocampus of chloral hydrate-anesthetized male rat. Systemic intravenous administration of duloxetine or fluoxetine inhibited dorsal raphe nucleus cell firing in a dose-dependent manner; duloxetine suppressed cell firing at significantly lower doses (ED100 1.4 +/- 0.3 mg/kg) than fluoxetine (ED100 10.0 +/- 2.0 mg/kg). In the hippocampus, microiontophoretic application of duloxetine or fluoxetine (0.01 M, pH 5.5; 5-40 nA) produced minimal inhibition of cell firing. When duloxetine was co-applied with 5-HT, the recovery response (RT50 values) of hippocampal pyramidal neurons to 5-HT application was not altered. In contrast, co-application of fluoxetine with 5-HT at the same iontophoretic currents significantly increased (59%) the RT50 values produced by 5-HT application alone. This physiological and pharmacological study contributes to understanding the cellular mechanisms of these agents which may be useful in the treatment of depression.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Analysis of Variance
  • Animals
  • Dose-Response Relationship, Drug
  • Duloxetine Hydrochloride
  • Electrophysiology
  • Fluoxetine / administration & dosage
  • Fluoxetine / pharmacology*
  • Fluoxetine / therapeutic use
  • Hippocampus / cytology
  • Hippocampus / drug effects*
  • Infusions, Intravenous
  • Iontophoresis
  • Male
  • Neurons / cytology
  • Neurons / drug effects
  • Raphe Nuclei / cytology
  • Raphe Nuclei / drug effects*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Serotonin / drug effects*
  • Receptors, Serotonin / metabolism
  • Receptors, Serotonin, 5-HT1
  • Selective Serotonin Reuptake Inhibitors / administration & dosage
  • Selective Serotonin Reuptake Inhibitors / pharmacology*
  • Selective Serotonin Reuptake Inhibitors / therapeutic use
  • Thiophenes / administration & dosage
  • Thiophenes / pharmacology*
  • Thiophenes / therapeutic use

Substances

  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • Serotonin Uptake Inhibitors
  • Thiophenes
  • Fluoxetine
  • Duloxetine Hydrochloride