Abstract
Stereo ( d and l), geometrical ( E and Z), and regiospecific (2-, 4-, and 6-[ 18F]fluoro) analogs of β-fluoromethylene- m-tyrosine (FMMT) have been investigated in adult vervet monkeys ( Cercopithecus aethiops sabaeus, n=12) in vivo with positron emission tomography (PET). Brain transport through the blood–brain barrier and central aromatic amino acid decarboxylase (AAAD)-mediated decarboxylation rates were established. Results show strict structural dependency of the kinetic behavior of radiofluorinated FMMT analogs, with the E-isomer exhibiting a higher specificity over the ( Z) geometrical counterpart for central dopaminergic structures. The 6-[ 18F]fluoro substituted l-( E)-FMMT was also favored over the 2- and 4-[ 18F]fluorosubstituted isomers in terms of their ability to localize in the same brain areas. The role of PET in drug development is also exemplified in this work.
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