کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373074 981888 2008 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Total synthesis and evaluation of [18F]MHMZ
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Total synthesis and evaluation of [18F]MHMZ
چکیده انگلیسی

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[18F]fluoroethyltosylate ([18F]FETos) was carried out in yields of ∼90% synthesizing [18F]MHMZ in a specific activity of ∼50 MBq/nmol with a starting activity of ∼3 GBq. Overall radiochemical yield including [18F]FETos synthon synthesis, [18F]fluoroalkylation and preparing the injectable [18F]MHMZ solution was 42% within a synthesis time of ∼100 min. The novel compound showed excellent specific binding to the 5-HT2A receptor (Ki = 9.0 nM) in vitro and promising in vivo characteristics.

The synthesis and evaluation of [18F]MHMZ, a potential 5-HT2A antagonist (Ki = 9.0 nM), is reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 4, 15 February 2008, Pages 1515–1519
نویسندگان
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