Discovery of [ 11 C]MK-8056: A Selective PET Imaging Agent for the Study of mGluR 2 Negative Allosteric Modulators

Modification of potent, selective metabotropic glutamate receptor 2 negative allosteric modulator (mGluR 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...

Full description

Saved in:
Bibliographic Details
Published in:ACS medicinal chemistry letters 2023-07, Vol.14 (7), p.986-992
Main Authors: Perkins, James J, McQuade, Paul, Bungard, Christopher J, Diamond, Tracy L, Gantert, Liza T, Gotter, Anthony L, Hanney, Barbara, Hills, Ivory D, Hurzy, Danielle M, Joshi, Aniket, Kern, Jonathan T, Schlegel, Kelly-Ann S, Manikowski, Jesse J, Meng, Zhaoyang, O'Brien, Julie A, Roecker, Anthony J, Smith, Sean M, Uslaner, Jason M, Hostetler, Eric, Meissner, Robert S
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Modification of potent, selective metabotropic glutamate receptor 2 negative allosteric modulator (mGluR 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 C or F radiolabel. [ C]MK-8056 was synthesized and evaluated and demonstrated appropriate affinity, selectivity, and physicochemical properties to be used as a positron emission tomography tracer for mGluR .
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.3c00175