Synthesis and preclinical evaluation of [¹¹C]MTP38 as a novel PET ligand for phosphodiesterase 7 in the brain.

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 [¹¹C]MTP38 as a novel positron emission tomography (PET) ligand for PDE7.

Methods

[¹¹C]MTP38 was radiosynthesized by ¹¹C-cyanation of a bromo precursor with [¹¹C]HCN. PET scans of rat and rhesus monkey brains and in vitro autoradiography of brain sections derived from these species were conducted with [¹¹C]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 stria

SUBMITTER: Obokata N 

PROVIDER: S-EPMC8426238 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature