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

doi:10.1039/C3MD00110E

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

Applied Medicine

Research output: Contribution to journal › Article › peer-review

13 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 language	English
Pages (from-to)	1118-1123
Number of pages	6
Journal	MedChemComm
Volume	4
Issue number	7
Early online date	29 May 2013
DOIs	https://doi.org/10.1039/C3MD00110E
Publication status	Published - 1 Jul 2013

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AU - Pratt, Judith A.

AU - Schweiger, Lutz Frank

AU - Pimlott, Sally

AU - Sutherland, Andrew

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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

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