| Literature DB >> 33418063 |
Yulong Xu1, Yiming Xu2, Hallie Blevins2, Yu Lan1, Yan Liu1, Gengyang Yuan3, Robin Striar1, Julia S Zagaroli1, Darcy R Tocci1, Amelia G Langan1, Can Zhang4, Shijun Zhang2, Changning Wang5.
Abstract
We report herein the discovery of a positron emission tomography (PET) tracer for the (NOD)-like receptor protein 3 (NLRP3). Our recent medicinal chemistry campaign on developing sulfonamide-based NLRP3 inhibitors led to an analog, 1, with a methoxy substituent amenable to labeling with carbon-11. PET/CT imaging studies indicated that [11C]1 exhibited rapid blood-brain barrier (BBB) penetration and moderate brain uptake, as well as blockable uptake in the brain. [11C]1, thus suggesting the potential to serve as a useful tool for imaging NLRP3 inflammasome in living brains.Entities:
Keywords: Blockable uptake; Blood-brain barrier (BBB) penetration; NLRP3; Positron emission tomography (PET); Sulfonamide derivative
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Year: 2021 PMID： 33418063 PMCID： PMC8785901 DOI： 10.1016/j.bmcl.2021.127777
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823