853760-23-3Relevant academic research and scientific papers
HETEROCYCLIC ACETOPHENONE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS
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Page/Page column 66, (2010/10/19)
The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy} phenyl)propanoic acid: A brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
Cube, Rowena V.,Vernier, Jean-Michel,Hutchinson, John H.,Gardner, Michael F.,James, Joyce K.,Rowe, Blake A.,Schaffhauser, Herve,Daggett, Lorrie,Pinkerton, Anthony B.
, p. 2389 - 2393 (2007/10/03)
We have identified and synthesized a brain penetrant propanoic acid as an allosteric potentiator of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency, level of potentiation and brain penetration led to the discovery of 8 (EC 50 = 1200 nM, 77% potentiation, 119% brain/plasma in rat, 20 mpk ip, brain level of 5700 nM).
