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Synthesis and Pharmacokinetic Study of a 11C-Labeled Cholesterol 24-Hydroxylase Inhibitor Using ‘In-Loop’ [11C]CO2 Fixation Method

submitted on 14.01.2020, 05:23 and posted on 22.01.2020, 05:38 by Zhen Chen, Jiahui Chen, Natalia Mast, Jian Rong, Xiaoyun Deng, Tuo Shao, Hualong Fu, Qingzhen Yu, Jiyun Sun, Yihan Shao, Lee Josephson, Thomas Lee Collier, Irina Pikuleva, Steven Liang

Cholesterol 24-hydroxylase is a monooxygenase encoded by CYP46A1, which is specifically expressed in the brain where it controls cholesterol elimination by producing 24S-hydroxylcholesterol (24-HC) as the major metabolite. Selective blockade of CYP46A1 activity may suppress neuronal cell death, Aβ deposition and p-tau accumulation by decreasing 24-HC formation, which thereafter serves as potential therapeutic pathway for Alzheimer’s disease. In this work, we showcase the efficient synthesis and preliminary pharmacokinetic evaluation of a novel cholesterol 24-hydroxylase inhibitor 1 by positron emission tomography study.


Email Address of Submitting Author


Massachusetts General Hospital and Harvard Medical School


United States

ORCID For Submitting Author


Declaration of Conflict of Interest

No conflict of interest