کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1393448 | 1501211 | 2008 | 5 صفحه PDF | دانلود رایگان |
5-HT3 receptor is an attractive target for the development of therapeutic agents for use in brain, heart and cancer diseases, and imaging agents for use in biomedical imaging technique PET. Benzoxazole derivatives are a novel class of 5-HT3 receptor partial agonists with high binding affinity. Carbon-11 labeled benzoxazole derivatives have been synthesized as new potential PET radioligands for imaging 5-HT3 receptor. The target tracers were prepared by N-[11C]methylation of their corresponding precursors using [11C]CH3OTf and isolated by HPLC purification procedure in 40–50% radiochemical yields, which were decay corrected to the end of bombardment (EOB), based on [11C]CO2. The overall synthesis time was 20–25 min from EOB. The radiochemical purity was >99%, and specific activity was in a range of 74–111 GBq/μmol at the end of synthesis (EOS).
This paper reports the synthesis of new carbon-11 labeled benzoxazole derivatives, potential PET radioligands for imaging 5-HT3 receptor.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 43, Issue 7, July 2008, Pages 1570–1574