Synthesis and in vitro evaluation of 18F labeled tyrosine derivatives as potential positron emission tomography (PET) imaging agents.
Three new 18F labeled fluoroalkyl tyrosine derivatives, O-(2-[18F]fluoroethyl)-alpha-methyltyrosine (FEMT, [18F]2), O-(2-[18F]fluoroethyl)-2-L-azatyrosine (FEAT, [18F]3), O-(2-[18F]fluoroethyl)-L-tyrosineamide (FETA, [18F]4) have been synthesized and radiofluorinated with 5-34% decay-corrected yield. In vitro studies were carried out in U-138 MG human glioblastoma. Cellular uptake of new tracers was compared to clinically utilized imaging agent O-(2-[18F]fluoroethyl)-L-tyrosine (FET, [18F]1). The uptake of tracers followed the order of FET ([18F]1) > FEAT([18F]3) > FEMT ([18F]2) approximately FETA ([18F]4).
Wang
Limin
L
Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104, USA.
Qu
Wenchao
W
Lieberman
Brian
B
Ploessl
Karl
K
Kung
Hank F
HF
D045744:Cell Line, Tumor; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics; D005909:Glioblastoma / Q000175:diagnosis; D006801:Humans; D007553:Isotope Labeling; D049268:Positron-Emission Tomography / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014443:Tyrosine / Q000031:analogs & derivatives / Q000493:pharmacokinetics
D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D014443:Tyrosine