Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor

Lynne Gilfillan, Adele Blair, Brian J. Morris, Judith A. Pratt, Lutz Frank Schweiger, Sally Pimlott, Andrew Sutherland

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Abstract

A focused library of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones containing sites for 11C-, 18F- and 123I-labelling have been prepared and evaluated against membrane expressing human recombinant metabotropic glutamate 2 receptor (mGluR2). The compounds were found to be non-competitive antagonists with nanomolar affinity. HPLC evaluation of the physiochemical properties of these compounds identified two candidates for PET and SPECT imaging of mGluR2.
Original languageEnglish
Pages (from-to)1118-1123
Number of pages6
JournalMedChemComm
Volume4
Issue number7
Early online date29 May 2013
DOIs
Publication statusPublished - 1 Jul 2013

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Gilfillan, L., Blair, A., Morris, B. J., Pratt, J. A., Schweiger, L. F., Pimlott, S., & Sutherland, A. (2013). Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor. MedChemComm, 4(7), 1118-1123. https://doi.org/10.1039/C3MD00110E