1242441-48-0Relevant articles and documents
Discovery of MK-3168: A PET tracer for imaging brain fatty acid amide hydrolase
Liu, Ping,Hamill, Terence G.,Chioda, Marc,Chobanian, Harry,Fung, Selena,Guo, Yan,Chang, Linda,Bakshi, Raman,Hong, Qingmei,Dellureficio, James,Lin, Linus S.,Abbadie, Catherine,Alexander, Jessica,Jin, Hong,Mandala, Suzanne,Shiao, Lin-Lin,Li, Wenping,Sanabria, Sandra,Williams, David,Zeng, Zhizhen,Hajdu, Richard,Jochnowitz, Nina,Rosenbach, Mark,Karanam, Bindhu,Madeira, Maria,Salituro, Gino,Powell, Joyce,Xu, Ling,Terebetski, Jenna L.,Leone, Joseph F.,Miller, Patricia,Cook, Jacquelynn,Holahan, Marie,Joshi, Aniket,O'Malley, Stacey,Purcell, Mona,Posavecz, Diane,Chen, Tsing-Bau,Riffel, Kerry,Williams, Mangay,Hargreaves, Richard,Sullivan, Kathleen A.,Nargund, Ravi P.,DeVita, Robert J.
, p. 509 - 513 (2013/07/26)
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. [11C]-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.