biostudies-literatureUnknown4(6)Liu PWe report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [(11)C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus monkeys and is a suitable PET tracer for imaging FAAH in the brain.ACS medicinal chemistry letters509-13https://www.ebi.ac.uk/biostudies/studies/S-EPMC4027136biostudies-literatureDiscovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.PMC4027136Riffel KWilliams MNargund RPGuo YLiu PWilliams DJochnowitz NFung SAlexander JMiller PAbbadie CPosavec DDeVita RJKaranam BSanabria SJin HSalituro GPowell JHamill TGHolahan MLeone JFChen TBMadeira MMandala SShiao LLBakshi RXu LChang LZeng ZO'Malley SRosenbach MJoshi ATerebetski JLChobanian HLi WCook JPurcell MChioda MLin LSHong QHargreaves RSullivan KADellureficio JHajdu RfalseDiscovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [(11)C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus monkeys and is a suitable PET tracer for imaging FAAH in the brain.2013-01-01T00:00:00Z2013 Jun2025-04-22T17:36:50.594Z2019-03-27T01:28:32ZS-EPMC40271362490070110.1021/ml4000996