کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1879481 | 1042573 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of one novel technetium-99m-labeled nitroquipazine derivative as an imaging agent for serotonin transporter
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
فیزیک و نجوم
تشعشع
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چکیده انگلیسی
Imaging of serotonin transporter (SERT) by positron emission tomography (PET) or single-photon emission-computed tomography (SPECT) in humans would provide useful information in diagnosis and therapy of several neurodegenerative and neuropsychiatric disorders. 6-Nitroquipazine is a highly potent and selective inhibitor of the SERT. For the development of new 99mTc-labeled 6-nitroquipazine derivatives as SERT imaging agents, novel [N-[2-((3-(4-(6-nitroquinolin-2-yl)piperazin-1-yl)propyl)(2-mercaptoethyl)amino]-acetyl-2-aminoethanethiolato] [99mTc]technetium (V) oxide (99mTc-MAMA-3-PQ) and its rhenium analog were synthesized and characterized. 99mTc-MAMA-3-PQ displayed high initial brain uptake (0.52% ID/organ at 2Â min post-injection (pi)) and relatively fast washout in mice (0.09% ID/organ at 60Â min pi). The regional brain distribution studies in rats showed high-specific binding ratios at 60Â min pi. Maximum regional contrast ratio observed for thalamus/cerebellum was 2.94, followed by 2.62 for hypothalamus/cerebellum. These encouraging results lead us to further explore its derivatives as new imaging agents for the SERT in the brain.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Applied Radiation and Isotopes - Volume 66, Issue 12, December 2008, Pages 1804-1809
Journal: Applied Radiation and Isotopes - Volume 66, Issue 12, December 2008, Pages 1804-1809
نویسندگان
Yunhang Guo, Xiangji Chen, Hongmei Jia, Xinmin Ji, Boli Liu,