Effects of sertraline and citalopram given repeatedly on the responsiveness of 5-HT receptor subpopulations

J Neural Transm Gen Sect. 1992;88(2):143-56. doi: 10.1007/BF01244819.


The effect of repeated treatment (5 and 10 mg/kg, po, twice daily, 14 days) with sertraline and citalopram (antidepressants which selectively inhibit the reuptake of 5-hydroxytryptamine (5-HT)) on the responsiveness of different 5-HT receptors to their agonists, was examined in rats and mice. Sertraline and citalopram (both at a dose 5 and 10 mg/kg) antagonized (the first one more potently) the hypothermia induced in mice by 8-OH-DPAT (a 5-HT1A agonist), but not the behavioural syndrome induced in rats by this substance. The m-chlorophenylpiperazine-induced hypothermia in mice (a 5-HT1B effect) was increased by sertraline and citalopram (only in a dose of 10 mg/kg). Both antidepressants, given repeatedly (as well acutely) attenuated exploratory hypoactivity induced in rats by m-chlorophenylpiperazine (a 5-HT1C effect). L-5-HTP-induced head twitches in mice (5-HT2 effect) were antagonized dose-dependently by both repeated sertraline and citalopram. Both antidepressants (citalopram only in higher dose) reduced the fenfluramine-induced hyperthermia in rats (5-HT2 effect). The results indicate that sertraline and citalopram given repeatedly decrease the responsiveness of 5-HT1A (presynaptic) and 5-HT2 receptors but increase the responsiveness of 5-HT1B receptors to respective agonists.

MeSH terms

  • 1-Naphthylamine / analogs & derivatives*
  • 1-Naphthylamine / pharmacology
  • 5-Hydroxytryptophan / pharmacology
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Animals
  • Behavior, Animal / drug effects
  • Body Temperature / drug effects
  • Citalopram / pharmacology*
  • Drug Interactions
  • Exploratory Behavior / drug effects
  • Fenfluramine / pharmacology
  • Male
  • Motor Activity / drug effects
  • Piperazines / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors
  • Receptors, Serotonin / drug effects*
  • Sertraline
  • Tetrahydronaphthalenes / pharmacology


  • Piperazines
  • Receptors, N-Methyl-D-Aspartate
  • Receptors, Serotonin
  • Tetrahydronaphthalenes
  • Citalopram
  • Fenfluramine
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • 1-Naphthylamine
  • 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid
  • 5-Hydroxytryptophan
  • Sertraline