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Synthesis and in vivo evaluation in mice of [123I]-(4-fluorophenyl)[1-(3-iodophenethyl)piperidin-4-yl]methanone as a potential SPECT-tracer for the serotonin 5-HT2A receptor

✍ Scribed by P. Blanckaert; I. Burvenich; F. Devos; G. Slegers

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
119 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

This work reports the synthesis, radiolabelling and in vivo evaluation in NMRI mice of [^123^I]‐(4‐fluorophenyl)[1‐(3‐iodophenethyl)piperidin‐4‐yl]methanone ([^123^I]‐3‐I‐CO) as a potential SPECT tracer for the 5‐HT~2A~ 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 [^123^I]‐3‐I‐CO as a 5‐HT~2A~ tracer. Copyright © 2007 John Wiley & Sons, Ltd.

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