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Synthesis, radiosynthesis and preliminary in vivo evaluation of [ 123 I]‐(4‐fluorophenyl) {1‐[2‐(2‐iodophenyl)ethyl]piperidin‐4‐yl}methanone, a potential 5‐HT 2A ‐antagonist for SPECT brain imaging
Author(s) -
Blanckaert P.,
Vandecapelle M.,
Staelens L.,
Burvenich I.,
Dierckx R. A.,
Slegers G.
Publication year - 2004
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.845
Subject(s) - radiosynthesis , chemistry , biodistribution , in vivo , antagonist , radioligand , chemical synthesis , ligand (biochemistry) , radiochemistry , specific activity , receptor , positron emission tomography , pharmacology , stereochemistry , nuclear medicine , in vitro , biochemistry , enzyme , medicine , microbiology and biotechnology , biology
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.