Issue 7, 2013
From the journal:

MedChemComm

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,a   Adele Blair,a   Brian J. Morris,b   Judith A. Pratt,c   Lutz Schweiger,d   Sally Pimlotte  and  Andrew Sutherland*a  

* Corresponding authors

a WestCHEM, School of Chemistry, The Joseph Black Building, University of Glasgow, Glasgow, UK
E-mail: Andrew.Sutherland@glasgow.ac.uk
Fax: +44 (0)141 330 4888
Tel: +44 (0)141 330 5936

b Institute of Neuroscience and Psychology, University of Glasgow, Glasgow, UK

c Centre for Neuroscience, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK

d John Mallard Scottish PET Centre, School of Medicine and Dentistry, University of Aberdeen, Foresterhill, Aberdeen, UK

e West of Scotland Radionuclide Dispensary, University of Glasgow and North Glasgow University Hospital NHS Trust, Glasgow, UK

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.

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

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Article information

DOI
https://doi.org/10.1039/C3MD00110E
Article type
Concise Article
Submitted
16 Apr 2013
Accepted
23 May 2013
First published
29 May 2013
This article is Open Access
Creative Commons BY license

Med. Chem. Commun., 2013,4, 1118-1123

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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

L. Gilfillan, A. Blair, B. J. Morris, J. A. Pratt, L. Schweiger, S. Pimlott and A. Sutherland, Med. Chem. Commun., 2013, 4, 1118 DOI: 10.1039/C3MD00110E

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