Preclinical development of [¹⁸F]TAAR1-2203 as a PET radioligand for imaging TAAR1 expression and receptor occupancy.

ABSTRACT:

Purpose

Trace amine-associated receptor 1 (TAAR1) is an emerging therapeutic target with various implications in neuropsychiatric and metabolic disorders. However, the absence of a suitable positron emission tomography (PET) radioligand has precluded non-invasive quantification of TAAR1 expression and drug-receptor interactions in vivo. In this study, we report the preclinical development of [¹⁸F]TAAR1-2203, a fluorine-18 labeled PET ligand suitable to image TAAR1 expression in peripheral tissues.

Methods

[¹⁸F]TAAR1-2203 ([¹⁸F]RO5263397) was obtained via copper-mediated radiofluorination. In vitro stability was assessed in formulation, serum and using liver microsomes. Specific binding was evaluated by in vitro autoradiography, ex vivo biodis

SUBMITTER: Haider A 

PROVIDER: S-EPMC12920416 | biostudies-literature | 2026 Mar

REPOSITORIES: biostudies-literature