Document Detail

Synthesis and biodistribution of [11C]adenosine 5'-monophosphate ([11C]AMP).
MedLine Citation:
PMID:  15912424     Owner:  NLM     Status:  MEDLINE    
PURPOSE: Imaging purine receptors and adenylate biodistribution in vivo may be of clinical importance not only for the investigation of normal adenylate metabolism but also in pathological conditions where adenylate uptake and/or release from certain tissues and organs may be altered, such as some types of cancer. In order to develop a tracer for positron emission tomography (PET) that would not be subject to loss of its radioisotope, adenosine 5'-monophosphate (AMP) was intrinsically labeled at the C-8 position with carbon-11. PROCEDURES: [11C]AMP was synthesized by reacting 5-amino-1-beta-D-ribofuranosylimidazole-4-carboxamidine-5'-phosphate with [11C]formaldehyde. The metabolism of [11C]AMP in human blood was determined in vitro both in the presence and absence of dipyridamole. The ex vivo biodistribution of [11C]AMP and its in vivo dosimetry were determined in normal mice. The effect of dipyridamole on the distribution of [11C]AMP in mice was also determined. RESULTS: [11C]AMP was reliably synthesized in 34 minutes (n = 7) with an average radiochemical yield of 2.4% and an average specific activity of 90.10 GBq/micromol (2435 mCi/micromol) at end of synthesis. In normal mice, the highest uptake of [11C]AMP was in the lungs, blood, and heart. The ex vivo mouse experiments showed that the uptake of 11C radiotracer in the lungs at 60 minutes postinjection was significantly lower for dipyridamole-treated animals than controls. Dosimetry showed that the critical organs for radiation dose burden are kidneys and bladder. CONCLUSIONS: Treatment with dipyridamole blocked the red blood cell uptake of extracellular adenosine and therefore its subsequent intracellular conversion to ATP. The biodistribution studies indicate that the tracer has substantial accumulation in the kidneys, lungs, heart, and blood. [11C]AMP is promising as a PET-imaging agent to trace adenylate biology in vivo.
William B Mathews; Yuji Nakamoto; Edward H Abraham; Ursula Scheffel; John Hilton; Hayden T Ravert; Mitsuaki Tatsumi; Paige A Rauseo; Bryan J Traughber; Anna Y Salikhova; Robert F Dannals; Richard L Wahl
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging     Volume:  7     ISSN:  1536-1632     ISO Abbreviation:  Mol Imaging Biol     Publication Date:    2005 May-Jun
Date Detail:
Created Date:  2005-05-24     Completed Date:  2005-09-19     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  101125610     Medline TA:  Mol Imaging Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  203-8     Citation Subset:  IM    
Division of Nuclear Medicine, Johns Hopkins University, Room B1151 Nelson Building, 600 N Wolfe St., Baltimore, MD 21287, USA.
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MeSH Terms
Adenosine Monophosphate / chemical synthesis*,  chemistry,  pharmacokinetics*
Carbon Radioisotopes
Chromatography, High Pressure Liquid
Dipyridamole / pharmacology
Molecular Structure
Grant Support
Reg. No./Substance:
0/Carbon Radioisotopes; 58-32-2/Dipyridamole; 61-19-8/Adenosine Monophosphate

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