Adenosine Receptor Ligands and PET Imaging of the CNS

Part of the Handbook of Experimental Pharmacology book series (HEP, volume 193)


Advances in radiotracer chemistry have resulted in the development of novel molecular imaging probes for adenosine receptors (ARs). With the availability of these molecules, the function of ARs in human pathophysiology as well as the safety and efficacy of approaches to the different AR targets can now be determined. Molecular imaging is a rapidly growing field of research that allows the identification of molecular targets and functional processes in vivo. It is therefore gaining increasing interest as a tool in drug development because it permits the process of evaluating promising therapeutic targets to be stratified. Further, molecular imaging has the potential to evolve into a useful diagnostic tool, particularly for neurological and psychiatric disorders. This chapter focuses on currently available AR ligands that are suitable for molecular neuroimaging and describes first applications in healthy subjects and patients using positron emission tomography (PET).


Adenosine receptors Brain disorders Drug development Molecular imaging Positron emission tomography Radioligands Radiosynthesis 



Adenosine monophosphate


Adenosine receptor


A1 adenosine receptor


A2A adenosine receptor


A2B adenosine receptor


A3 adenosine receptor


Alzheimer’s disease


(E)-8-(3-Bromostyryl)-3,7-dimethyl- 1-propargylxanthine




Central nervous system




(E)-8-Chlorostyryl-1,3,7-trimethylxanthine (8-chlorostyrylcaffeine)


Dopamine D2 receptor






50% Efficient dose






5-(2-[18F]fluoroethyl)-2,4-diethyl-3-(ethylsulfa- nylcarbonyl)-6-phenylpyridine-5-carboxylate


2-(1-Methyl-4-piperidinyl)-6-(2-phenylpyrazolo [1,5-a]pyridin-3-yl)-3(2H)-pyridazinone


(E)-3,7-Dimethyl-8-(3-iodostyryl)-1- propargylxanthine


Kiloelectron volt






(E)-8-(3,4-Dimethoxystyryl)-1,3-dipropyl-7- methylxanthine

KF18446 (TMSX)

(E)-8-(3,4,5-Trimethoxystyryl)-1,3,7- trimethylxanthine


(E)-1,3-Diallyl-7-methyl-8-(3,4,5-trimethoxystyryl) xanthine


(E)-8-(2,3-Dimethyl-4-methoxystyryl)-1,3, 7-trimethylxanthine


3-[1-(6,7-Dimethoxyquinazolin-4-yl)piperidin-4-yl]-1, 6-dimethyl-2, 4(1H, 3H)-quinazolinedione

KW-6002 (istradefylline)

(E)1,3-Diethyl-8-(3,4-dimethoxystyryl)- 7-methylxanthine


Positron emission tomography


Parkinson’s disease



SCH 58261

7-(2-Phenylethyl)-5-amino-2-(2-furyl)-pyrazolo [4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine


Single-photon emission computed tomography


Standard uptake value




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© Springer-Verlag Berlin Heidelberg 2009

Authors and Affiliations

  1. 1.Institute of Neuroscience and Biophysics (INB-3)Research Center JülichJülichGermany
  2. 2.Positron Medical Center, Tokyo Metropolitan Institute of GerontologyItabashiJapan

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