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Discovery of [11C]MK-8056: A Selective PET Imaging Agent for the Study of mGluR2 Negative Allosteric Modulators.
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.
Afiliação
  • Perkins JJ; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • McQuade P; Translational Imaging, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Bungard CJ; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Diamond TL; Pharmacology, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Gantert LT; Translational Imaging, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Gotter AL; Neuroscience Biology Discovery, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Hanney B; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Hills ID; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Hurzy DM; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Joshi A; Translational Imaging, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Kern JT; Neuroscience Biology Discovery, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Schlegel KS; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Manikowski JJ; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Meng Z; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • O'Brien JA; Pharmacology, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Roecker AJ; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Smith SM; Neuroscience Biology Discovery, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Uslaner JM; Neuroscience Biology Discovery, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Hostetler E; Translational Imaging, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
  • Meissner RS; Departments of Discovery Chemistry, Merck & Co., Inc., 770 Sumneytown Pike, PO Box 4, West Point, Pennsylvania 19486, USA.
ACS Med Chem Lett ; 14(7): 986-992, 2023 Jul 13.
Article em En | MEDLINE | ID: mdl-37465306
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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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Estados Unidos