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
P. Blanckaert, M. Vandecapelle, L. Staelens
Aug 1, 2004
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Journal of Labelled Compounds and Radiopharmaceuticals
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Key Takeaway Key Takeaway: The 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
Abstract
Many people suffer from psychiatric illnesses like depression and anorexia. Relevant to these diseases is amongst others a malfunctioning of brain 5-HT2A-receptors. To allow in vivo quantification of these receptors with Single Photon Emission Computerized Tomography (SPECT), a radiolabelled ligand with high 5-HT2A affinity is needed. This work reports the radiosynthesis of [123I]-(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.