Automated Synthesis and Initial Evaluation of (4'-Amino-5',8'-difluoro-1'H-spiro[piperidine-4,2'-quinazolin]-1-yl)(4-[¹⁸F]fluorophenyl)methanone for PET/MR Imaging of Inducible Nitric Oxide Synthase.

ABSTRACT:

Background

Inducible nitric oxide synthase (iNOS) plays a crucial role in neuroinflammation, especially microglial activity, and may potentially represent a useful biomarker of neuroinflammation. In this study, we carefully defined a strategic plan to develop iNOS-targeted molecular PET imaging using (4'-amino-5',8'-difluoro-1'H-spiro[piperidine-4,2'-quinazolin]-1-yl)(4-fluorophenyl)methanone ([¹⁸F]FBAT) as a tracer in a mouse model of lipopolysaccharide- (LPS-) induced brain inflammation.

Methods

An in vitro model, murine microglial BV2 cell line, was used to assess the uptake of [¹⁸F]FBAT in response to iNOS induction at the cellular level. In vivo whole-body dynamic PET/MR imaging was acquired in LPS-treated (5 mg/kg) and control mice.

SUBMITTER: Yeh SH 

PROVIDER: S-EPMC8328489 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature