کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1379404 982027 2005 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents
چکیده انگلیسی

A series of fluoro substituted aryl carboxamides was synthesized revealing high affinity for the dopamine D3 receptor. In contrast to 2-methoxy substitution, a 2,3-dichloro substitution pattern at the phenylpiperazine moiety induces a 10-fold increase of D3 affinity which is expressed by Ki values of 0.53, 1.1, and 9.0 nM for 8b, 8d, and 8f. Applying aromatic 18F-for-Br(Cl) substitution, high radiochemical yields between 76–82% were obtained for [18F]8c–f. The most promising ligand, [18F]8d, was used as imaging agent of the D3 receptor in vitro. However, due to the lack of specific binding, further studies should aim at the development of radioligands with improved D3 receptor selectivity.

A series of dopamine D3 receptor radioligands were synthesized. The 6-fluoropyridin-3-yl derivative [18F]8d displayed good D3 affinity (Ki = 1.1 nM) and was used for receptor autoradiography studies on rat brain slices.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 21, 1 November 2005, Pages 4819–4823
نویسندگان
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