Adenosine A(2A) receptor antagonists as Positron Emission Tomography (PET) tracers.
The adenosine A(2A) receptor (A(2A)R) 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(2A)R 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(2A)R PET ligands is available. The present article has been therefore focused on available PET tracers for A(2A)R 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(2A)Rs is discussed in the present article. A brief overview of functions of adenosine in health and disease, including the relevance of A(2A)R for PD has also been presented.
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S
Khanapur
A van
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Waarde
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K
Ishiwata
K L
KL
Leenders
R A J O
RA
Dierckx
Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Hanzeplein 1, 9713GZ Groningen, The Netherlands. shivakhanapur4u@gmail.com.
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PH
Elsinga
D058917:Adenosine A2 Receptor Antagonists / Q000737:chemistry*; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D006801:Humans; D062105:Molecular Docking Simulation; D010300:Parkinson Disease / Q000000981:diagnostic imaging; D049268:Positron-Emission Tomography / Q000379:methods*; D043705:Receptor, Adenosine A2A / Q000032:analysis*; D014970:Xanthines / Q000737:chemistry
D058917:Adenosine A2 Receptor Antagonists; D043705:Receptor, Adenosine A2A; D014970:Xanthines