335349-65-0Relevant academic research and scientific papers
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,Pimlott, Sally,Sutherland, Andrew
, p. 1118 - 1123 (2013/07/26)
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.
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: New potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1
Woltering, Thomas J.,Adam, Geo,Alanine, Alexander,Wichmann, Juergen,Knoflach, Frederic,Mutel, Vincent,Gatti, Silvia
, p. 6811 - 6815 (2008/04/03)
A series of 1,3-dihydrobenzo[b][1,4]diazepin-2-one derivatives was evaluated as non-competitive mGluR2/3 antagonists. Attachment of an 8-(2-aryl)-ethynyl-moiety produced compounds inhibiting the binding of [3H]-LY354740 to rat mGluR2 with low n
Glutamate receptor antagonists
-
, (2008/06/13)
The present invention relates to compounds of with a base structure of formula 1 The compounds of formula I are shown to have activity as metabotropic glutamate receptor antagonists.
