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5-HT 1A  receptors have been implicated in the pathogenesis of a wide variety of disorders related to the serotonin receptors. WAY100635 is a well-known high affinity 5-HT 1A  receptor antagonist. Many  11 C and  18 F radiolabeled derivatives and its radioiodinated analogues have been reported as imaging agents for 5-HT 1A  receptors. In this regard, the synthesis, radiolabeling and biological evaluation of a new 5-HT 1A  receptor radioligand, [ 125 I]-1-(2-(benzylthio)ethyl)-4-(5-iodo-2-methoxyphenyl)piperazine ([ 125 I]-BTE-IMPP), are described. Radioiodination of this newly synthesized compound was done by the direct aromatic electrophilic substitution  via  Iodo-Gen method. Radiochemical yield and radiochemical purity determined by TLC and RTLC were &gt;70% and &gt;95%, respectively. Biodistribution studies of [ 125 I]-BTE-IMPP in rats displayed relatively high uptake in hippocampus (Hip) and low uptake in cerebellum (Cer). The level of the radiotracer uptake was over threefold higher in hippocampus than in cerebellum at 30 min post-injection. Moreover, the brain to blood uptake ratio and the blocking studies results indicated prolonged retention of the radiotracer and relatively good specific binding to 5-HT 1A  receptor. These findings strongly suggest that [ 125 I]-BTE-IMPP could be a good candidate as an  in vivo  marker for pharmacological study of 5-HT 1A  receptors in animal models.

radiochimica acta

Synthesis, radiolabeling and biological evaluation of [ 125 I]-1-[2-(benzylthio)ethyl]-4-(5-iodo-2-methoxyphenyl)piperazine as a new 5-HT 1A  receptor ligand