Adenosine A_2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers

Title:Adenosine A_2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers

Volume: 21 Issue: 3

Author(s): S. Khanapur, A. van Waarde, K. Ishiwata, K. L. Leenders, R. A.J.O. Dierckx and P. H. Elsinga

Affiliation:

Keywords: Adenosine A_2A receptor, Parkinson’s disorder, positron emission tomography (PET), xanthine ligands, nonxanthine ligands, SCH442416, TMSX, 6-OHDA PD model.

Abstract: The adenosine A_2A receptor (A_2AR) is highly concentrated in the striatum, and a therapeutic target for Parkinson’s disorder (PD) and Huntington’s disease. High affinity and selective radiolabeled A_2AR antagonists can be important research and diagnostic tools for PD. Positron Emission Tomography (PET) can play an important role by measuring radiolabeled A_2A antagonists non-invasively in the brain. However, till date no complete review on A_2AR PET ligands is available. The present article has been therefore focused on available PET tracers for A_2AR 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 A_2ARs is discussed in the present article. A brief overview of functions of adenosine in health and disease, including the relevance of A_2AR for PD has also been presented.

Cite this article as:

Khanapur S., Waarde van A., Ishiwata K., Leenders L. K., Dierckx A.J.O. R. and Elsinga H. P., Adenosine A_2A Receptor Antagonists as Positron Emission Tomography (PET) Tracers, Current Medicinal Chemistry 2014; 21 (3) . https://dx.doi.org/10.2174/09298673113206660265