Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
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ABSTRACT:
SUBMITTER: Liu P
PROVIDER: S-EPMC4027136 | biostudies-other | 2013 Jun
REPOSITORIES: biostudies-other
Publications
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Liu Ping P Hamill Terence G TG Chioda Marc M Chobanian Harry H Fung Selena S Guo Yan Y Chang Linda L Bakshi Raman R Hong Qingmei Q Dellureficio James J Lin Linus S LS Abbadie Catherine C Alexander Jessica J Jin Hong H Mandala Suzanne S Shiao Lin-Lin LL Li Wenping W Sanabria Sandra S Williams David D Zeng Zhizhen Z Hajdu Richard R Jochnowitz Nina N Rosenbach Mark M Karanam Bindhu B Madeira Maria M Salituro Gino G Powell Joyce J Xu Ling L Terebetski Jenna L JL Leone Joseph F JF Miller Patricia P Cook Jacquelynn J Holahan Marie M Joshi Aniket A O'Malley Stacey S Purcell Mona M Posavec Diane D Chen Tsing-Bau TB Riffel Kerry K Williams Mangay M Hargreaves Richard R Sullivan Kathleen A KA Nargund Ravi P RP DeVita Robert J RJ
ACS medicinal chemistry letters 20130420 6
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 ...[more]
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