Discovery of carbon-11 labeled sulfonamide derivative: A PET tracer for imaging brain NLRP3 inflammasome

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 [C-11]1 exhibited rapid blood-brain barrier (BBB) penetration and moderate brain uptake, as well as blockable uptake in the brain. [C-11]1, thus suggesting the potential to serve as a useful tool for imaging NLRP3 inflammasome in living brains.

Automated summary

The newly discovered PET tracer [C-11]1 showed rapid penetration of the blood-brain barrier and blockable uptake in the brain, indicating its potential as a useful tool for imaging NLRP3 inflammasome in living brains.