335353-01-0Relevant academic research and scientific papers
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 2. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists
Woltering, Thomas J.,Adam, Geo,Wichmann, Juergen,Goetschi, Erwin,Kew, James N.C.,Knoflach, Frederic,Mutel, Vincent,Gatti, Silvia
, p. 1091 - 1095 (2008/09/20)
A series of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives was evaluated as non-competitive mGluR2/3 antagonists. Replacement of a cyano group by a five-membered heterocycle produced compounds inhibiting the binding of [3H]-LY354740 to rat mGluR2 with low nanomolar affinity and consistent functional effect at both mGluR2 and mGluR3. Further modification to improve the physicochemical properties led eventually to compounds with the ability to reverse LY354740-mediated inhibition of field excitatory postsynaptic potentials in the rat dentate gyrus.
Glutamate receptor antagonists
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, (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.
