Synthesis and in vivo evaluation in mice of (123l)-(4-fluorophenyl)(l-(3-iodophenethyl)piperidin-4-yl) methanone as a potential SPECT-tracer for the serotonin 5-HT2a receptor

摘要

This work reports the synthesis, radiolabelling and in vivo evaluation in NMRI mice of [123I]-{4-fluorophenyl)[l-(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 lOmin 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.