123I-5-I-R91150, a new single-photon emission tomography ligand for 5-HT2A receptors: influence of age and gender in healthy subjects |
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Authors: | Chris Baeken Hugo D’haenen Patrick Flamen John Mertens Dirk Terriere Kris Chavatte Rony Boumon Axel Bossuyt |
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Institution: | (1) Department of Psychiatry, Academic Hospital, Brussels, Belgium, BE;(2) Department of Nuclear Medicine, Academic Hospital, Brussels, Belgium, BE;(3) Cyclotron Unit, Free University of Brussels, Brussels, Belgium, BE |
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Abstract: | 5-HT2A receptors have been implicated in the pathophysiology of mood disorders and in the therapeutic effect of the so-called atypical
antipsychotics. Recently, a new radioiodinated ligand with high affinity and selectivity for serotonin 5-HT2A receptors, 123iodinated 4-amino-N-1-3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl] 5-iodo-2-methoxybenzamide (123I-5-I-R91150), has been developed and has been shown to be suitable for single-photon emission tomography (SPET) imaging.
In this study the influence of age and gender on the ligand binding was investigated in normal volunteers. One hundred and
fifty MBq of 123I-5-I-R91150 was administered to 26 normal volunteers (13 females and 13 males) with an age range of 23–60 years. SPET imaging
was performed with a triple-headed gamma camera. For semi-quantitative analysis, ratios of ligand binding in different regions
of interest to the binding in the cerebellum were calculated. Mean ratios of 1.7 were obtained. No gender difference was demonstrated.
5-HT2A binding was shown to decline with age. Over an age range of 40 years a reduction in ligand binding of 42%±7% was found. These
results are in agreement with in vitro and positron emission tomography findings of a decline in 5-HT2A receptor binding with age. The findings confirm the suitability of 123I-5-I-R91150 for SPET imaging of 5-HT2A receptors, and highlight the necessity for age-matched controls in clinical studies.
Received 21 March and in revised form 18 August 1998 |
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Keywords: | : 5-HT2A receptors New tracer 123I-5-I-R91150 Single-photon emission tomography |
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