synthesis and biological evaluation of 99mtc(co)3-oh-pp-cs2 for brain receptor imaging

introduction: 5-ht1a receptor is related with a variety of neuropsychiatric disorders. . in this study a phenolic analogue derived from dway [desmethyl way-100635 (n-(2-(1-(4-(2-methoxyphenyl)piperazinyl)-ethyl))-n-(2-pyridinyl) cyclohexanecarboxamide)] is used to design the desired structure of 5-ht1a receptor imaging agents after labeling with [99mtc (co) 3(h2o) 3] + core via dithiocarbamate moiety. methods: 2-(piperazin-1-yl) phenol dithiocarbamate was synthesized by the reaction of 2-(piperazin-1-yl) phenol with an equivalent amount of carbon disulfide in koh solution then radiolabeled with [99mtc(co)3(h2o)3]+ core. radioligand chemical analysis involved high-performance liquid chromatography methods. radioconjugate stability and lipophilicity were determined. biodistribution of labeled compound was studied in rats. results: the final complex was characterized by hplc and its radiochemical purity was more than 90%. in vitro stability studies have shown the complex was stable at least 6-hrs after labeling at room temperature. the n-octanol/water partition coefficient experiment demonstrated log p = 0.74 for 99mtc(co)3-oh-pp-cs2. biodistribution results showed that radio tracer had moderate brain uptake (0.32 ± 0.03 %id/g at 30 min post injection), conclusion: this complex may lead to a further development of a radiotracer with specific binding to 5-ht1a receptor.