Development of a Novel ¹⁸F-Labeled Radioligand for Imaging Cholesterol 24-Hydroxylase with Positron Emission Tomography.

ABSTRACT: Cholesterol 24-hydroxylase (CYP46A1), also known as CH24H, is a brain-specific monooxygenase responsible for the elimination of cholesterol from the central nervous system (CNS). It catalyzes the conversion of cholesterol to 24(S)-hydroxycholesterol, the primary pathway for CNS cholesterol clearance. Dysregulation of cholesterol homeostasis has been implicated in neurodegenerative diseases, such as Alzheimer's disease (AD) and Parkinson's disease (PD). This study presents the synthesis and evaluation of [¹⁸F]5 ([¹⁸F]CHL2310) as a novel radioligand for imaging CYP46A1 and cholesterol metabolism in the brain by positron emission tomography (PET). CHL2310 was identified as a potent inhibitor of CYP46A1 and subsequently labeled with fluorine-18 in a radioche

SUBMITTER: Rong J 

PROVIDER: S-EPMC11915032 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature