%0 Journal Article
%T Synthesis and Biological Evaluation of 99mTc(CO)3-OH-PP-CS2 for Brain Receptor Imaging
%A Mostafa Erfani
%A Leila Hassanzadeh
%A Seyed Esmaeil Sadat Ebrahimi
%A Mohammad Shafiei
%J Iranian Journal of Nuclear Medicine
%D 2012
%I 
%X 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 ¡À 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.
%K Serotonin
%K 99mTc-Carbonyl
%K DWAY
%K Brain Imaging
%U http://irjnm.tums.ac.ir/?_action=showPDF&article=1209&_ob=ea5ebb2b7402c6a5baf4af65b1abfc9c&fileName=full_text.pdf