TY - JOUR
T1 - Synthesis of 2′-fluoro-5-[11C]-methyl-1-β-d-arabinofuranosyluracil ([11C]-FMAU)
T2 - A potential nucleoside analog for in vivo study of cellular proliferation with PET
AU - Conti, Peter S.
AU - Alauddin, Mian M.
AU - Fissekis, John R.
AU - Schmall, Bernard
AU - Watanabe, Kyochi A.
PY - 1995/8
Y1 - 1995/8
N2 - 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.
AB - 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.
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U2 - 10.1016/0969-8051(95)00017-R
DO - 10.1016/0969-8051(95)00017-R
M3 - Article
C2 - 8535339
AN - SCOPUS:0029064884
SN - 0969-8051
VL - 22
SP - 783
EP - 789
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
IS - 6
ER -