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Adenosine Receptor Ligands and PET Imaging of the CNS

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Adenosine Receptors in Health and Disease

Part of the book series: Handbook of Experimental Pharmacology ((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).

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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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Authors and Affiliations

  1. Institute of Neuroscience and Biophysics (INB-3), Research Center Jülich, 52425, Jülich, Germany

    Andreas Bauer

  2. Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, 1-1, Nakacho, Itabashi, Tokyo, 173-0011, Japan

    Kiichi Ishiwata

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  1. Andreas Bauer
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Correspondence to Andreas Bauer .

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  1. Endacea, Inc.,, Davis Drive 2, Research Triangle Park, 27709-2076, U.S.A.

    Constance N. Wilson

  2. Health Sciences Center, West Virginia University, Health Sciences S. 2267, Morgantown, 26506-9104, U.S.A.

    S. Jamal Mustafa

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Bauer, A., Ishiwata, K. (2009). Adenosine Receptor Ligands and PET Imaging of the CNS. In: Wilson, C., Mustafa, S. (eds) Adenosine Receptors in Health and Disease. Handbook of Experimental Pharmacology, vol 193. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-89615-9_19

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