Description:
<jats:p>The present study evaluated the tumoral uptake of the novel synthetic amino acid positron emission tomography (PET) tracers (S)‐2‐amino‐3‐(4‐([<jats:sup>18</jats:sup>F]fluoromethyl)‐1<jats:italic>H</jats:italic>‐1,2,3‐triazol‐1‐yl)propanoic acid (AMC‐101), (S)‐2‐amino‐4‐(4‐([<jats:sup>18</jats:sup>F]fluoromethyl)‐1<jats:italic>H</jats:italic>‐1,2,3‐triazol‐1‐yl)butanoic acid (AMC‐102), and (S)‐2‐amino‐5‐(4‐([<jats:sup>18</jats:sup>F]fluoromethyl)‐1<jats:italic>H</jats:italic>‐1,2,3‐triazol‐1‐yl)pentanoic acid (AMC‐103), all of which are (<jats:italic>S</jats:italic>)‐2‐amino‐(4‐([<jats:sup>18</jats:sup>F]fluoromethyl)‐1<jats:italic>H</jats:italic>‐1,2,3‐triazol‐1‐yl)alkyl acids. <jats:italic>In vitro</jats:italic> cellular uptake was investigated using the rat glioma cell lines 9L and C6. <jats:italic>In vitro</jats:italic> competitive inhibition tests were performed to identify the involvement of specific amino acid transporters. <jats:italic>In vivo</jats:italic> dynamic PET images of 9L xenograft tumor‐bearing model mice were acquired over 2 h after AMC administration. [<jats:sup>18</jats:sup>F]FDOPA PET studies were performed with and without S‐carbidopa pretreatment for comparison. All three AMCs exhibited good <jats:italic>in vitro</jats:italic> cell uptake through the L and alanine‐serine‐cysteine transporters and enabled clear tumor visualization on PET, leaving the brain devoid of the tracer. Thirty minutes after injection, the mean tumor standardized uptake values were 1.59 ± 0.05, 1.89 ± 0.27, and 1.74 ± 0.13 for AMC‐101, AMC‐102, and AMC‐103, respectively. Although the tumor uptake values of AMCs were lower than that of [<jats:sup>18</jats:sup>F]FDOPA with S‐carbidopa pretreatment, AMCs enabled higher contrast images with lower background activity compared with [<jats:sup>18</jats:sup>F]FDOPA with S‐carbidopa pretreatment. Our results indicate the potential uses of these new synthetic amino acids as oncologic radiotracers.</jats:p>