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Synthesis, radiosynthesis and preliminary in vivo evaluation of [123I]-(4-fluorophenyl) {1-[2-(2-iodophenyl)ethyl]piperidin-4-yl}methanone, a potential 5-HT2A-antagonist for SPECT brain imaging

✍ Scribed by P. Blanckaert; M. Vandecapelle; L. Staelens; I. Burvenich; R. A. Dierckx; G. Slegers

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
106 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Many people suffer from psychiatric illnesses like depression and anorexia. Relevant to these diseases is amongst others a malfunctioning of brain 5‐HT~2A~‐receptors. To allow in vivo quantification of these receptors with Single Photon Emission Computerized Tomography (SPECT), a radiolabelled ligand with high 5‐HT~2A~ affinity is needed.

This work reports the radiosynthesis of [^123^I]‐(4‐fluorophenyl) {1‐[2‐(2‐iodophenyl)ethyl]piperidin‐4‐yl}methanone, the synthesis of its precursor, (4‐fluorophenyl) {1‐[2‐(2‐bromophenyl)ethyl]piperidin‐4‐yl}methanone, and the preliminary in vivo evaluation of the tracer. The precursor was synthesized with a total yield of 40%. Radiolabelling was performed using a halogen exchange reaction and the yield was 70%. Radiochemical purity was >95%, and specific activity was at least 2.4 Ci/µmol. Log P was measured to be 2.52. The tracer showed uptake in mice brain (3.5% I.D./g tissue at 3 min post injection) and therefore will be evaluated further by regional brain biodistribution and displacement studies in rabbits. Copyright © 2004 John Wiley & Sons, Ltd.

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