P. Blanckaert, I. Burvenich, F. Devos
Mar 15, 2007
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Influential Citations
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Quality indicators
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
This work reports the synthesis, radiolabelling and in vivo evaluation in NMRI mice of [123I]-(4-fluorophenyl)[1-(3-iodophenethyl)piperidin-4-yl]methanone ([123I]-3-I-CO) as a potential SPECT tracer for the 5-HT2A receptor. The tributylstannylprecursor was synthesized with a 15% overall yield. Radiolabelling was performed using an electrophilic iododestannylation with yields of 85%. Radiochemical purity was always >95%. Log P was determined to be 3.10±0.10. The tracer showed good uptake in mouse brain (6.3±1.3% ID/g tissue at 10 min p.i., 2±0.36% ID/g tissue at 1 h p.i.). These results warrant further research in larger animals to determine suitability of [123I]-3-I-CO as a 5-HT2A tracer. Copyright © 2007 John Wiley & Sons, Ltd.