W. J. Behof, C. Whitmore, J. Haynes
Jan 31, 2022
Citations
0
Influential Citations
4
Citations
Journal
FEBS Letters
Abstract
L‐ergothioneine (ERGO) is a potent antioxidant with cytoprotective effects. To study ERGO biodistribution and detect oxidative stress in vivo, we report an efficient and reproducible preparation of [11C]‐labeled ERGO PET radioligand based on protecting the histidine carboxylic group with a methyl ester. Overall, this new protection approach using methyl ester improved the chemical yield of a 4‐step reaction from 14% to 24% compared to the previous report using t‐butyl ester. The [11C]CH3 methylation of the precursor provided the desired product with 55 ± 10% radiochemical purity and a molar activity of 450 ± 200 TBq·mmol−1. The [11C]ERGO radioligand was able to detect threshold levels of oxidative stress in a preclinical animal model of Alzheimer’s disease.