856256-81-0Relevant articles and documents
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents
Engers, Julie L.,Rodriguez, Alice L.,Konkol, Leah C.,Morrison, Ryan D.,Thompson, Analisa D.,Byers, Frank W.,Blobaum, Anna L.,Chang, Sichen,Venable, Daryl F.,Loch, Matthew T.,Niswender, Colleen M.,Daniels, J. Scott,Jones, Carrie K.,Conn, P. Jeffrey,Lindsley, Craig W.,Emmitte, Kyle A.
, p. 7485 - 7500 (2015)
Previous preclinical work has demonstrated the therapeutic potential of antagonists of the group II metabotropic glutamate receptors (mGlus). Still, compounds that are selective for the individual group II mGlus (mGlu2 and mGlu3) hav
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency
Turlington, Mark,Noetzel, Meredith J.,Bridges, Thomas M.,Vinson, Paige N.,Steckler, Thomas,Lavreysen, Hilde,Mackie, Claire,Bartolomé-Nebreda, José M.,Conde-Ceide, Susana,Tong, Han Min,Macdonald, Gregor J.,Daniels, J. Scott,Jones, Carrie K.,Niswender, Colleen M.,Conn, P. Jeffrey,Lindsley, Craig W.,Stauffer, Shaun R.
, p. 3641 - 3646 (2014/07/22)
We report the optimization of a series of novel metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from a 5,6-bicyclic class of dihydropyrazolo[1,5-a]pyridin-4(5H)-ones containing a phenoxymethyl linker. Studies foc
SUBSTITUTED BICYCLIC ARALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Paragraph 00574; 00400, (2014/01/09)
In one aspect, the invention relates to substituted bicyclic aralkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
