⁶⁸ Ga-Labelled Tropane Analogues for the Visualization of the Dopaminergic System.

ABSTRACT: The development of radiometal-labelled pharmaceuticals for neuroimaging could offer great potential due to easier handling during labelling and availability through radionuclide generator systems. Nonetheless, to date, no such tracers are available for positron emission tomography, primarily owing to the challenge of crossing the blood-brain barrier (BBB) and loss of affinity through chelator attachment. We have prepared a variety of ⁶⁸ Ga-labelled phenyltropanes showing that, through a simple hydrocarbon-linker, it is possible to introduce a chelator onto the lead structure while maintaining its high affinity for hDAT (human dopamine transporter) and simultaneously achieving adequate lipophilicity. One of the candidates, [⁶⁸ Ga]Ga-HBED-hexadiyne-tropane, showed an IC

SUBMITTER: Haseli S 

PROVIDER: S-EPMC7984292 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature