کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362960 | 981500 | 2010 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists](/preview/png/1362960.png)
Movement disorders such as Parkinson’s disease and Huntington’s disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, that is, the A2A AR. To further this goal, we have synthesized and characterized pharmacologically a family of high affinity A2A AR ligands, based on the known antagonist, SCH 442416 (R = –Me), which have structural variability on the terminus (R = –Et, –i-Pr, –allyl, and others). A O-fluoroethyl analogue suitable for use as a PET tracer had a Ki value of 12.4 nM and was highly selective for the A2A AR in comparison to the A1 and A3 ARs.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 19, 1 October 2010, Pages 5690–5694