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Discovery of [11C]MK-8056: A Selective PET Imaging Agent for the Study of mGluR2 Negative Allosteric Modulators

James J. Perkins,Paul McQuade,Christopher J. Bungard,Tracy L. Diamond,Liza Gantert,Anthony L. Gotter,Barbara Hanney, Ivory D. Hills, Danielle M. Hurzy,Aniket Joshi, Jonathan T. Kern, Kelly-Ann S. Schlegel,Jesse J. Manikowski,Zhaoyang Meng,Julie A. O’Brien,Anthony J. Roecker, Sean M. Smith,Jason M. Uslaner,Eric D. Hostetler,Robert Meißner

ACS Medicinal Chemistry Letters（2023）

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Abstract
Modification of potent, selective metabotropic glutamate receptor 2 negative allosteric modulator (mGluR2 NAM) led to a series of analogues with excellent binding affinity, lipophilicity, and suitable physicochemical properties for a PET tracer with convenient chemical handles for incorporation of a 11C or 18F radiolabel. [11C]MK-8056 was synthesized and evaluated in vivo and demonstrated appropriate affinity, selectivity, and physicochemical properties to be used as a positron emission tomography tracer for mGluR2.
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selective pet imaging agent,mglur<sub>2</sub>
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