Easily automated radiosynthesis of [¹⁸F]P10A-1910 and its clinical translation to quantify phosphodiesterase 10A in human brain.

ABSTRACT: Our previous work showed that [¹⁸F]P10A-1910 was a potential radioligand for use in imaging phosphodiesterase 10A (PDE10A). Specifically, it had high brain penetration and specific binding that was demonstrated in both rodents and non-human primates. Here, we present the first automatic cGMP-level production of [¹⁸F]P10A-1910 and translational PET/MRI study in living human brains. Successful one-step radiolabeling of [¹⁸F]P10A-1910 on a GE TRACERlab FX2N synthesis module was realized via two different methods. First, formulated [¹⁸F]P10A-1910 was derived from heating spirocyclic iodonium ylide in a tetra-n-butyl ammonium methanesulfonate solution. At the end of synthesis, it was obtained in non-decay corrected radiochemical yields (n.d.c.

SUBMITTER: Wei H 

PROVIDER: S-EPMC9486304 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature