Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase
- ACS Med Chem Lett. 2013 Apr 20;4(6):509-13. doi: 10.1021/ml4000996.
- 1. Departments of Medicinal Chemistry, Immunology, Pharmacology, Preclinical DMPK, Basic Pharmaceutical Sciences, and Process Research, Merck Research Laboratories , Rahway, New Jersey 07065, United States.
- 2. Department of Imaging Research, Merck Research Laboratories , West Point, Pennsylvania 19486, United States.
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.
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Cat. No.Product NameDescriptionTargetResearch Area
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Research Areas: Metabolic Disease
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target: FAAHResearch Areas: Neurological Disease