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Adenosine A2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers

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The adenosine A2A receptor (A2AR) is highly concentrated in the striatum, and a therapeutic target for Parkinson’s disorder (PD) and Huntington’s disease. High affinity and selective radiolabeled A2AR antagonists can be important research and diagnostic tools for PD. Positron Emission Tomography (PET) can play an important role by measuring radiolabeled A2A antagonists non-invasively in the brain. However, till date no complete review on A2AR PET ligands is available. The present article has been therefore focused on available PET tracers for A2AR and their detailed biological evaluation in rodents, nonhuman primates and humans. Drug design and development by molecular modeling including new lead structures that are potential candidates for radiolabeling and mapping of cerebral A2ARs is discussed in the present article. A brief overview of functions of adenosine in health and disease, including the relevance of A2AR for PD has also been presented.

Keywords: 6-OHDA PD model; Adenosine A2A receptor; Parkinson’s disorder; SCH442416; TMSX; nonxanthine ligands; positron emission tomography (PET); xanthine ligands

Document Type: Research Article

Publication date: January 1, 2014

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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