The effects of paroxetine given repeatedly on the 5-HT receptor subpopulations in the rat brain

Psychopharmacology (Berl). 1996 Sep;127(1):73-82. doi: 10.1007/BF02805977.

Abstract

Effects of paroxetine (10 mg/kg PO, twice daily, 14 days) on 5-HT receptor subpopulations in the brain were evaluated pharmacologically, electrophysiologically and biochemically in male Wistar rats. Imipramine was used for comparison. Repeated paroxetine antagonized the 8-OH-DPAT-induced behavioural syndrome (a 5-HT1A effect); imipramine showed similar, yet weaker, activity. The 5-HT-or 8-OH-DPAT-induced inhibition of population spikes in hippocampal slices was increased by both those repeated antidepressants. Repeated (or acute) paroxetine decreased the density of and increased the affinity for 5-HT1A receptors ([3H]-8-OH-DPAT used as ligand) in the hippocampus, while imipramine induced opposite effects. m-Chlorophenyl piperazine (m-CPP)-evoked exploratory hypoactivity, a 5-HT2C effect, was reduced by repeated paroxetine, but not by imipramine. Either of the antidepressants given repeatedly antagonized TFMPP-induced hyperthermia (another putative 5-HT2C effect). 5-HTP-induced head twitches (a 5-HT2A effect) were inhibited by repeated paroxetine or imipramine. Either antidepressant given repeatedly decreased the density of 5-HT2A receptors ([3H]-ketanserin as a ligand) in the brain cortex, but did not change their affinity. The present results indicate that paroxetine given repeatedly induces secondary changes in 5-HT2 receptors, which lead to reduction of the 5-HT2 neurotransmission (reduced responsiveness of 5-HT2 postsynaptic receptors). The consequences of the secondary changes in 5-HT1A receptors, found here still await clarification.

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
  • Animals
  • Behavior, Animal / drug effects
  • Brain Chemistry / drug effects*
  • Electrophysiology
  • Hippocampus / chemistry
  • Imipramine / pharmacology
  • Male
  • Motor Activity / drug effects
  • Paroxetine / pharmacology*
  • Piperazines / pharmacology
  • Rats
  • Rats, Wistar
  • Receptors, Serotonin / analysis*
  • Receptors, Serotonin / drug effects
  • Selective Serotonin Reuptake Inhibitors / pharmacology*
  • Serotonin Receptor Agonists / pharmacology

Substances

  • Piperazines
  • Receptors, Serotonin
  • Serotonin Receptor Agonists
  • Serotonin Uptake Inhibitors
  • 1-(3-trifluoromethylphenyl)piperazine
  • Paroxetine
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Imipramine