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, L., Blair, A., Morris, B. , Pratt, J., Schweiger, L., Pimlott, S. and 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), pp. 1118-1123. (doi:10.1039/c3md00110e)

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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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Pimlott, Dr Sally and Sutherland, Dr Andrew and Haahr, Dr Lynne and Pratt, Dr Judith and Morris, Professor Brian
Authors: Gilfillan, L., Blair, A., Morris, B., Pratt, J., Schweiger, L., Pimlott, S., and Sutherland, A.
College/School:College of Medical Veterinary and Life Sciences > Institute of Neuroscience and Psychology
College of Medical Veterinary and Life Sciences > School of Medicine, Dentistry & Nursing
College of Science and Engineering > School of Chemistry
Journal Name:MedChemComm
Publisher:Royal Society of Chemistry
ISSN:2040-2503
ISSN (Online):2040-2511
Copyright Holders:Copyright © 2013 The Authors
First Published:First published in MedChemComm 4(7):1118-1123
Publisher Policy:Reproduced under a Creative Commons License

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