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.
Appl Radiat Isot
; 62(5): 737-43, 2005 May.
Article
en En
| MEDLINE
| ID: mdl-15763480
ABSTRACT
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.
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Bases de datos:
MEDLINE
Asunto principal:
Piperidinas
/
Tomografía Computarizada de Emisión de Fotón Único
/
Radiofármacos
/
Receptor de Serotonina 5-HT2A
Límite:
Animals
Idioma:
En
Revista:
Appl Radiat Isot
Asunto de la revista:
MEDICINA NUCLEAR
/
SAUDE AMBIENTAL
Año:
2005
Tipo del documento:
Article
País de afiliación:
Bélgica