A radioligand for in vitro autoradiography of CSF1R in post-mortem CNS tissues.

ABSTRACT:

Background

Reactive microglia and recruited peripheral macrophages contribute to the pathogenesis of Alzheimer's dementia (AD). Monocytes, macrophages and microglia all express the marker colony-stimulating factor 1 receptor (CSF1R). 4-Cyano-N-(4-(4-methylpiperazin-1-yl)-2-(4-methylpiperidin-1-yl)phenyl)-1H-pyrrole-2-carboxamide (1) is a high-affinity antagonist for CSF1R. We report the radiosynthesis of both [³H]1 and [¹¹C]1. The PET imaging properties of [¹¹C]1 in mice and baboon were investigated. [³H]1 was studied in B_max measurement in post-mortem autoradiography in the frontal cortex, inferior parietal cortex and hippocampus from donors diagnosed with AD and age-matched controls. In vitro binding affinity of 1 was measure

SUBMITTER: Foss CA 

PROVIDER: S-EPMC11347546 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature