Adenosine Receptor Ligands and PET Imaging of the CNS

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

Abstract

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).

Keywords

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

Abbreviations

AMP

Adenosine monophosphate

AR

Adenosine receptor

A1AR

A1 adenosine receptor

A2AAR

A2A adenosine receptor

A2BAR

A2B adenosine receptor

A3AR

A3 adenosine receptor

AD

Alzheimer’s disease

BS–DMPX

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

Bq

Becquerel

CNS

Central nervous system

CPFPX

8-Cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine

CSC

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

D2R

Dopamine D2 receptor

DMPX

3,7-Dimethyl-1-propylxanthine

DPCPX

8-Cyclopentyl-1,3-dipropylxanthine

ED50

50% Efficient dose

EPDX

2-Ethyl-8-dicyclopropylmethyl-3-propylxanthine

FDG

2-Deoxy-2-fluoro-d-glucose

[18F]FE@SUPPY

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

FR194921

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

IS–DMPX

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

keV

Kiloelectron volt

KF15372

8-Dicyclopropylmethyl-1,3-dipropylxanthine

MPDX

8-Dicyclopropylmethyl-1-methyl-3-propylxanthine

KF17837

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

KF18446 (TMSX)

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

KF19631

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

KF21213

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

KF21652

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

PET

Positron emission tomography

PD

Parkinson’s disease

SCH442416

5-Amino-7-(3-(4-methoxyphenyl)propyl)-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine

SCH 58261

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

SPECT

Single-photon emission computed tomography

SUV

Standard uptake value

Sv

Sievert

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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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