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Decreased [18F]MPPF Binding Potential in the Dorsal Raphe Nucleus After a Single Oral Dose of Fluoxetine: A Positron-Emission Tomography Study in Healthy Volunteers
- Source :
-
Biological Psychiatry . Jun2008, Vol. 63 Issue 12, p1135-1140. 6p. - Publication Year :
- 2008
-
Abstract
- Background: Brain serotonin-1A (5-HT1A) autoreceptors internalize when activated by agonist or by their endogenous ligand, serotonin. This positron-emission tomography (PET) study tested the hypothesis that 5-HT1A autoreceptor internalization might be indexed in vivo by a decrease in the specific binding of the 5-HT1A radioligand, 4-[18F]fluoro-N-[2-[1-(2-methoxyphenyl)-1 piperazinyl]ethyl-N-2-pyridinyl-benzamide ([18F]MPPF), in the dorsal raphe nucleus (DRN) of healthy adult men administered a single oral dose of the selective serotonin reuptake inhibitor, fluoxetine. Methods: [18F]MPPF binding potential was measured in the DRN and other brain regions endowed with 5-HT1A receptors in eight healthy volunteers, 5 hours after the randomized, double-blind administration of fluoxetine (20 mg) or placebo. Results: In every subject, [18F]MPPF binding potential was decreased in the DRN only (44% ± 22 SD), in response to fluoxetine. Conclusions: Imaging the functional state of 5-HT1A autoreceptors (i.e., internalization) in the human brain, using [18F]MPPF/PET, may represent a promising avenue for investigating the neurobiology of serotonin-related disorders and notably of major depression. [Copyright &y& Elsevier]
- Subjects :
- *SEROTONIN
*LIGANDS (Biochemistry)
*AUTORECEPTORS
*NEUROTRANSMITTERS
Subjects
Details
- Language :
- English
- ISSN :
- 00063223
- Volume :
- 63
- Issue :
- 12
- Database :
- Academic Search Index
- Journal :
- Biological Psychiatry
- Publication Type :
- Academic Journal
- Accession number :
- 32495885
- Full Text :
- https://doi.org/10.1016/j.biopsych.2007.11.016