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 Schweiger, Sally Pimlott, Andrew Sutherland*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Downloads (Pure)

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
Early online date29 May 2013
DOIs
Publication statusPublished - 1 Jul 2013

Keywords

  • organic chemistry
  • medicinal chemistry
  • medical imaging

Fingerprint

Dive into the research topics of 'Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor'. Together they form a unique fingerprint.

Cite this