» Articles » PMID: 18373090

Biodistribution and Radiation Dosimetry of the A1 Adenosine Receptor Ligand 18F-CPFPX Determined from Human Whole-body PET

Overview
Date 2008 Apr 1
PMID 18373090
Citations 7
Authors
Affiliations
Soon will be listed here.
Abstract

Purpose: (18)F-8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ((18)F-CPFPX) is a potent radioligand to study human cerebral A(1) adenosine receptors and their neuromodulatory and neuroprotective functions with positron emission tomography (PET). The purpose of this study was to determine the biodistribution and the radiation dose of (18)F-CPFPX by whole-body scans in humans.

Methods: Six normal volunteers were examined with 12 whole-body PET scans from 1.5 min to 4.5 h after injection. Volumes of interest were defined over all visually identifiable organs, i.e. liver, gallbladder, kidneys, small intestines, heart, and brain to obtain the organs' volumes and time-activity curves (TACs). TACs were fitted with exponential functions, extrapolated, multiplied with the physical decay and normalized to injected activities so that the residence times could be computed as area under the curve. Radiation doses were calculated using the OLINDA/EXM software for internal dose assessment in nuclear medicine.

Results: The liver uptake shows peak values (decay-corrected) of up to 35% of the injected radioactivity. About 30% is eliminated by bladder voiding. The highest radiation dose is received by the gallbladder (136.2 +/- 66.1 muSv/MBq), followed by the liver (84.4 +/- 10.6 muSv/MBq) and the urinary bladder (78.3 +/- 7.1 muSv/MBq). The effective dose was 17.6 +/- 0.5 muSv/MBq.

Conclusions: With 300 MBq of injected (18)F-CPFPX a subject receives an effective dose (ICRP 60) of 5.3 mSv. Thus the effective dose of an (18)F-CPFPX study is comparable to that of other (18)F-labelled neuroreceptor ligands.

Citing Articles

Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications.

Zarrinmayeh H, Territo P Mol Imaging. 2020; 19:1536012120927609.

PMID: 32539522 PMC: 7297484. DOI: 10.1177/1536012120927609.


An one-pot two-step automated synthesis of [18F]T807 injection, its biodistribution in mice and monkeys, and a preliminary study in humans.

Huang Y, Chiu M, Yen R, Tsai C, Hsieh H, Chiu C PLoS One. 2019; 14(7):e0217384.

PMID: 31260447 PMC: 6602418. DOI: 10.1371/journal.pone.0217384.


An Optimized MicroPET Imaging Method for the Distribution and Synergies of Natural Products.

Cui Q, Liu Y, Zhou M, Han Y, Yin C, Bai G Front Pharmacol. 2018; 9:948.

PMID: 30186178 PMC: 6110851. DOI: 10.3389/fphar.2018.00948.


Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging.

Pike V Curr Med Chem. 2016; 23(18):1818-69.

PMID: 27087244 PMC: 5579844. DOI: 10.2174/0929867323666160418114826.


Biodistribution and radiation dosimetry of the integrin marker 18F-RGD-K5 determined from whole-body PET/CT in monkeys and humans.

Doss M, Kolb H, Zhang J, Belanger M, Stubbs J, Stabin M J Nucl Med. 2012; 53(5):787-95.

PMID: 22499613 PMC: 7607669. DOI: 10.2967/jnumed.111.088955.


References
1.
Svenningsson P, Hall H, Sedvall G, Fredholm B . Distribution of adenosine receptors in the postmortem human brain: an extended autoradiographic study. Synapse. 1998; 27(4):322-35. DOI: 10.1002/(SICI)1098-2396(199712)27:4<322::AID-SYN6>3.0.CO;2-E. View

2.
Meyer P, Elmenhorst D, Bier D, Holschbach M, Matusch A, Coenen H . Quantification of cerebral A1 adenosine receptors in humans using [18F]CPFPX and PET: an equilibrium approach. Neuroimage. 2005; 24(4):1192-204. DOI: 10.1016/j.neuroimage.2004.10.029. View

3.
Meyer P, Elmenhorst D, Zilles K, Bauer A . Simplified quantification of cerebral A1 adenosine receptors using [18F]CPFPX and PET: analyses based on venous blood sampling. Synapse. 2005; 55(4):212-23. DOI: 10.1002/syn.20113. View

4.
Herzog H, Zilken H, Niederbremer A, Friedrich W . Calculation of residence times and radiation doses using the standard PC software Excel. Eur J Nucl Med. 1998; 24(12):1514-21. DOI: 10.1007/s002590050182. View

5.
Holschbach M, Olsson R, Bier D, Wutz W, Sihver W, Schuller M . Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. J Med Chem. 2002; 45(23):5150-6. DOI: 10.1021/jm020905i. View