PMCCPMCCPMCC

Search tips
Search criteria 

Advanced

 
Logo of jpnSubmit a ManuscriptEmail AlertsAbout JPNJournal of Psychiatry and Neuroscience
 
J Psychiatry Neurosci. 1994 January; 19(1): 63–67.
PMCID: PMC1188564

Effects of repeated treatment with fluoxetine and citalopram, 5-HT uptake inhibitors, on 5-HT1A and 5-HT2 receptors in the rat brain.

Abstract

Repeated treatment with fluoxetine and citalopram, which are potent 5-HT reuptake inhibitors, resulted in different regulation of 5-HT1A and 5-HT2 receptors in the rat brain. Their effects were compared with those of other antidepressants: imipramine, mianserin and levoprotiline. The density of 5-HT1A receptors, labelled with [3H]8-OH-DPAT, in the rat hippocampus was enhanced after citalopram, imipramine, mianserin and levoprotiline, but not altered after fluoxetine administration. [3H]Ketanserin binding sites, which label 5-HT2 receptors, were increased after fluoxetine and levoprotiline, but decreased after citalopram, imipramine and mianserin in the rat cerebral cortex. Acute administration of fluoxetine, but not citalopram, resulted in a decreased density of 5-HT1A receptors. 5-HT2 receptors were not changed by acute administration of either fluoxetine or citalopram. The obtained results indicate that besides 5-HT reuptake inhibiting properties of both compounds, there may exist an additional mechanism(s) of their action, which leads to different regulation of 5-HT1A and 5-HT2 receptors.

Full text

Full text is available as a scanned copy of the original print version. Get a printable copy (PDF file) of the complete article (763K), or click on a page image below to browse page by page. Links to PubMed are also available for Selected References.

Selected References

These references are in PubMed. This may not be the complete list of references from this article.
  • Arnt J, Hyttel J, Overø KF. Prolonged treatment with the specific 5-HT-uptake inhibitor citalopram: effect on dopaminergic and serotonergic functions. Pol J Pharmacol Pharm. 1984 Mar-Jun;36(2-3):221–230. [PubMed]
  • Caldecott-Hazard S, Morgan DG, DeLeon-Jones F, Overstreet DH, Janowsky D. Clinical and biochemical aspects of depressive disorders: II. Transmitter/receptor theories. Synapse. 1991 Dec;9(4):251–301. [PubMed]
  • Cervo L, Samanin R. Potential antidepressant properties of 8-hydroxy-2-(di-n-propylamino)tetralin, a selective serotonin1A receptor agonist. Eur J Pharmacol. 1987 Dec 1;144(2):223–229. [PubMed]
  • Cheetham SC, Crompton MR, Katona CL, Horton RW. Brain 5-HT1 binding sites in depressed suicides. Psychopharmacology (Berl) 1990;102(4):544–548. [PubMed]
  • Conn PJ, Sanders-Bush E. Central serotonin receptors: effector systems, physiological roles and regulation. Psychopharmacology (Berl) 1987;92(3):267–277. [PubMed]
  • de Montigny C, Aghajanian GK. Tricyclic antidepressants: long-term treatment increases responsivity of rat forebrain neurons to serotonin. Science. 1978 Dec 22;202(4374):1303–1306. [PubMed]
  • Goodwin GM, Green AR, Johnson P. 5-HT2 receptor characteristics in frontal cortex and 5-HT2 receptor-mediated head-twitch behaviour following antidepressant treatment to mice. Br J Pharmacol. 1984 Sep;83(1):235–242. [PubMed]
  • Green AR. Evolving concepts on the interactions between antidepressant treatments and monoamine neurotransmitters. Neuropharmacology. 1987 Jul;26(7B):815–822. [PubMed]
  • Green AR, Heal DJ, Johnson P, Laurence BE, Nimgaonkar VL. Antidepressant treatments: effects in rodents on dose-response curves of 5-hydroxytryptamine- and dopamine-mediated behaviours and 5-HT2 receptor number in frontal cortex. Br J Pharmacol. 1983 Oct;80(2):377–385. [PubMed]
  • Kellar KJ, Cascio CS, Butler JA, Kurtzke RN. Differential effects of electroconvulsive shock and antidepressant drugs on serotonin-2 receptors in rat brain. Eur J Pharmacol. 1981 Feb 19;69(4):515–518. [PubMed]
  • Kennett GA, Dourish CT, Curzon G. Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression. Eur J Pharmacol. 1987 Feb 24;134(3):265–274. [PubMed]
  • Leysen JE. Gaps and peculiarities in 5-HT2 receptor studies. Neuropsychopharmacology. 1990 Oct-Dec;3(5-6):361–369. [PubMed]
  • Leysen JE, Niemegeers CJ, Van Nueten JM, Laduron PM. [3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role. Mol Pharmacol. 1982 Mar;21(2):301–314. [PubMed]
  • Maj J, Moryl E. Effects of sertraline and citalopram given repeatedly on the responsiveness of 5-HT receptor subpopulations. J Neural Transm Gen Sect. 1992;88(2):143–156. [PubMed]
  • Maj J, Moryl E. Effects of fluoxetine given chronically on the responsiveness of 5-HT receptor subpopulations to their agonists. Eur Neuropsychopharmacol. 1993 Jun;3(2):85–94. [PubMed]
  • Mann JJ, Arango V, Marzuk PM, Theccanat S, Reis DJ. Evidence for the 5-HT hypothesis of suicide. A review of post-mortem studies. Br J Psychiatry Suppl. 1989 Dec;(8):7–14. [PubMed]
  • Mogilnicka E, Klimek V. Mianserin, danitracen and amitriptyline withdrawal increases the behavioural responses of rats to L-5-HTP. J Pharm Pharmacol. 1979 Oct;31(10):704–705. [PubMed]
  • Peroutka SJ, Snyder SH. Long-term antidepressant treatment decreases spiroperidol-labeled serotonin receptor binding. Science. 1980 Oct 3;210(4465):88–90. [PubMed]
  • Schlegel JR, Peroutka SJ. Nucleotide interactions with 5-HT1A binding sites directly labeled by [3H]-8-hydroxy-2-(DI-n-propylamino)tetralin ([3H]-8-OH-DPAT). Biochem Pharmacol. 1986 Jun 15;35(12):1943–1949. [PubMed]
  • Tatarczyńska E, Chojnacka-Wójcik E. Effects of 8-OH-DPAT and ipsapirone in the tests used for evaluation of the antidepressant action. Pol J Pharmacol Pharm. 1989 Jul-Aug;41(4):321–330. [PubMed]
  • van Praag HM, Korf J. A pilot study of some kinetic aspects of the metabolism of 5-hydroxytryptamine in depressive patients. Biol Psychiatry. 1971;3(2):105–112. [PubMed]
  • Vetulani J, Lebrecht U, Pilc A. Enhancement of responsiveness of the central serotonergic system and serotonin-2 receptor density in rat frontal cortex by electroconvulsive treatment. Eur J Pharmacol. 1981 Nov 19;76(1):81–85. [PubMed]
  • Welner SA, De Montigny C, Desroches J, Desjardins P, Suranyi-Cadotte BE. Autoradiographic quantification of serotonin1A receptors in rat brain following antidepressant drug treatment. Synapse. 1989;4(4):347–352. [PubMed]
  • Willner P. Antidepressants and serotonergic neurotransmission: an integrative review. Psychopharmacology (Berl) 1985;85(4):387–404. [PubMed]
  • Wong DT, Fuller RW, Robertson DW. Fluoxetine and its two enantiomers as selective serotonin uptake inhibitors. Acta Pharm Nord. 1990;2(3):171–180. [PubMed]
  • Yates M, Leake A, Candy JM, Fairbairn AF, McKeith IG, Ferrier IN. 5HT2 receptor changes in major depression. Biol Psychiatry. 1990 Mar 1;27(5):489–496. [PubMed]

Articles from Journal of Psychiatry & Neuroscience : JPN are provided here courtesy of Canadian Medical Association