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

Research output: Contribution to journalArticle

8 Citations (Scopus)

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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Imaging techniques
Single-Photon Emission-Computed Tomography
Labeling
Libraries
High Pressure Liquid Chromatography
Membranes
1,5-benzodiazepin-2-one
metabotropic glutamate receptor 2

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Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor. / Gilfillan, Lynne; Blair, Adele ; Morris, Brian J.; Pratt, Judith A.; Schweiger, Lutz Frank; Pimlott, Sally; Sutherland, Andrew .

In: MedChemComm, Vol. 4, No. 7, 01.07.2013, p. 1118-1123.

Research output: Contribution to journalArticle

Gilfillan, Lynne ; Blair, Adele ; Morris, Brian J. ; Pratt, Judith A. ; Schweiger, Lutz Frank ; Pimlott, Sally ; Sutherland, Andrew . / Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor. In: MedChemComm. 2013 ; Vol. 4, No. 7. pp. 1118-1123.
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