Psychopharmacology

, Volume 144, Issue 3, pp 279–281

The effects of single dose nefazodone and paroxetine upon 5-HT2A binding potential in humans using [18F]-setoperone PET

  • J. H. Meyer
  • R. Cho
  • S. Kennedy
  • S. Kapur
ORIGINAL INVESTIGATION

DOI: 10.1007/s002130051004

Cite this article as:
Meyer, J., Cho, R., Kennedy, S. et al. Psychopharmacology (1999) 144: 279. doi:10.1007/s002130051004

Abstract

Rationale: Alterations in 5-HT2A receptor binding are implicated in suicidality and depression. 5-HT2A receptors may also be involved in the therapeutic effects of antidepressants. Objectives: The purpose of this study was to assess the effect of paroxetine and nefazodone on 5-HT2A receptors after a single dose. Methods: Seven subjects received a single dose of nefazodone 200 mg and five subjects received a single dose of paroxetine 20 mg. Before and after the dose, 5-HT2A binding potentials (Bmax/Kd) were determined in each subject using [18F]-setoperone PET. Results: Nefazodone induced a significant change in 5-HT2A binding potential (−39 ± 17%, P = 0.003) while paroxetine showed no significant alteration of 5-HT2A binding potential (+3 ± 13%, P = 0.73). Conclusions: The change in 5-HT2A binding potential seen with nefazodone represents blockade of 5-HT2A receptors by the drug. We do not find evidence for acute downregulation of 5-HT2A receptors with paroxetine within 9 h.

Key words Serotonin 5-HT2 receptor Selective serotonin reuptake inhibitors Positron emission tomography Depression Antidepressant 

Copyright information

© Springer-Verlag Berlin Heidelberg 1999

Authors and Affiliations

  • J. H. Meyer
    • 1
  • R. Cho
    • 2
  • S. Kennedy
    • 3
  • S. Kapur
    • 2
  1. 1.The Mood and Anxiety Division and PET Centre, The Clarke Division of the Centre for Addictions and Mental Health, 250 College St., Toronto, Ontario, Canada M5T 1R8CA
  2. 2.Schizophrenia Division, The Clarke Division of the Centre for Addictions and Mental Health, 250 College St., Toronto, Ontario, Canada M5T 1R8 e-mail: kapur@clarke-inst.on.ca Fax: +1-416-979-4656CA
  3. 3.The Mood and Anxiety Division, The Clarke Division of the Centre for Addictions and Mental Health, 250 College St., Toronto, Ontario, Canada M5T 1R8CA

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