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• W3097156576 abstract "Abstract Purpose Phosphodiesterase (PDE) 7 is a potential therapeutic target for neurological and inflammatory diseases, although in-vivo visualization of PDE7 has not been successful. In this study, we aimed to develop [ 11 C]MTP38 as a novel positron emission tomography (PET) ligand for PDE7. Methods [ 11 C]MTP38 was radiosynthesized by 11 C-cyanation of a bromo precursor with [ 11 C]HCN. PET scans of rat and rhesus monkey brains and in-vitro autoradiography of brain sections derived from these species were conducted with [ 11 C]MTP38. In monkeys, dynamic PET data were analyzed with an arterial input function to calculate the total distribution volume ( V T ). The non-displaceable binding potential ( BP ND ) in the striatum was also determined by a reference tissue model with cerebellar reference. Finally, striatal occupancy of PDE7 by an inhibitor was calculated in monkeys according to changes in BP ND . Results [ 11 C]MTP38 was synthesized with radiochemical purity ≥ 99.4% and molar activity of 38.6 ± 12.6 GBq/μmol. Autoradiography revealed high radioactivity in the striatum and its reduction by non-radiolabeled ligands, in contrast with unaltered autoradiographic signals in other regions. In-vivo PET after radioligand injection to rats and monkeys demonstrated that radioactivity was rapidly distributed to the brain and intensely accumulated in the striatum relative to the cerebellum. Correspondingly, estimated V T values in the monkey striatum and cerebellum were 3.59 and 2.69 mL/cm 3 , respectively. The cerebellar V T value was unchanged by pretreatment with unlabeled MTP38. Striatal BP ND was reduced in a dose-dependent manner after pretreatment with MTP-X, a PDE7 inhibitor. Relationships between PDE7 occupancy by MTP-X and plasma MTP-X concentration could be described by Hill’s sigmoidal function. Conclusion We have provided the first successful preclinical demonstration of in-vivo PDE7 imaging with a specific PET radioligand. [ 11 C]MTP38 is a feasible radioligand for evaluating PDE7 in the brain and is currently being applied to a first-in-human PET study." @default.
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• W3097156576 date "2020-10-29" @default.
• W3097156576 modified "2023-10-17" @default.
• W3097156576 title "Synthesis and preclinical evaluation of [11C]MTP38 as a novel PET ligand for phosphodiesterase 7 in the brain" @default.
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• W3097156576 doi "https://doi.org/10.1101/2020.10.29.354696" @default.
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