Synthesis, radiosynthesis and in vivo evaluation in mice of [123I]-(4-fluorophenyl) {1-[2-(4-iodophenyl)ethyl]piperidin-4-yl}methanone for visualization of the 5-HT2A receptor with SPECT.
This work reports the synthesis, radiolabelling and preliminary in vivo evaluation of [(123)I]-(4-fluorophenyl){1-[2-(4-iodophenyl)ethyl]piperidin-4-yl}methanone. The tributylstannylprecursor was synthesized with a yield of 30%. Radiolabelling was performed using an electrophilic iododestannylation. Tracer yield was 80%, radiochemical purity was >95% and specific activity was at least 55 Ci/micromol. Log P was 1.5. The tracer showed uptake in mice brain (2.72% ID/g tissue at 5 min p.i.) and therefore will be evaluated further by regional brain biodistribution and displacement studies in rabbits.
Blanckaert
P
P
Laboratory for Radiopharmacy, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium. peter.blanckaert@ugent.de
Burvenich
I
I
Staelens
L
L
Dierckx
R A
RA
Slegers
G
G
D000818:Animals; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
C502122:(123I)-(4-fluorophenyl)(1-(2-(4-iodophenyl)ethyl)piperidin-4-yl)methanone; D010880:Piperidines; D019275:Radiopharmaceuticals; D044402:Receptor, Serotonin, 5-HT2A