| Abstract: |
Rapid in vivo catabolism limits the use of currently available radiotracers used in tumor proliferation studies with PET. This is manifested by the need to develop complex mathematical models to interpret kinetic and metabolite data obtained from imaging studies with agents such as carbon-11 labeled thymidine. A potential carbon-11 labeled radiotracer for cellular proliferation, 2′-fluoro-5-([11C]-methyl)-1-β-d-arabinofuranosyluracil (FMAU), has been prepared using a previously described method for preparation of [11dmethyl-thymidine where selective alkylation of a pyrimidyl dianion is accomplished with [11C]methyl iodide at the 5-position of the pyrimidine ring. FMAU shares many in vivo characteristics of thymidine, including cellular transport, phosphorylation by mammalian kinase, and incorporation into DNA. Most importantly, in vivo catabolism of FMAU is limited, potentially yielding simplified kinetic models for determination of cellular proliferation with positron emission tomography. © 1995. |
| Keywords: |
controlled study; positron emission tomography; methodology; cell proliferation; animal; animals; cell division; drug synthesis; models, theoretical; kinetics; diagnostic agent; isotope labeling; computer assisted emission tomography; drug derivative; uracil arabinoside; arabinofuranosyluracil; theoretical model; synthesis; carbon; tomography, emission-computed; indicators and reagents; carbon 11; dyes, reagents, indicators, markers and buffers; clevudine; carbon radioisotopes; humans; human; article; 2'-fluoro-5-methylarabinosyluracil
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