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Iranian Journal of Nuclear Medicine، جلد ۲۰، شماره ۱، صفحات ۲۵-۳۱
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عنوان انگلیسی Synthesis and biological evaluation of 99mTc(CO)3-OH-PP-CS2 for brain receptor imaging
چکیده انگلیسی مقاله 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.
کلیدواژه‌های انگلیسی مقاله Serotonin,99mTc-carbonyl,DWAY,Brain imaging
نویسندگان مقاله مصطفی عرفانی |
nuclear science research school, nuclear science and technology research institute, atomic energy organization of iran, tehran, iran
سازمان اصلی تایید شده: سازمان انرژی اتمی (Atomic energy organization)

لیلا حسن زاده |
department of nuclear pharmacy, faculty of pharmacy, tehran university of medical sciences, tehran, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

سید اسماعیل سادات ابراهیمی | seyed esmaeil sadat ebrahimi
department of medicinal chemistry, faculty of pharmacy, tehran university of medical sciences, tehran, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی تهران (Tehran university of medical sciences)

محمد شفیعی |
nuclear science research school, nuclear science and technology research institute, atomic energy organization of iran, tehran, iran
سازمان اصلی تایید شده: سازمان انرژی اتمی (Atomic energy organization)

نشانی اینترنتی http://irjnm.tums.ac.ir/article_1209_ea5ebb2b7402c6a5baf4af65b1abfc9c.pdf
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