353232-77-6Relevant academic research and scientific papers
Potentiators of glutamate receptors
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Page 33, (2010/02/05)
The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same.
SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide
Barda, David A.,Wang, Zhao-Qing,Britton, Thomas C.,Henry, Steven S.,Jagdmann, G. Erik,Coleman, Darrell S.,Johnson, Michael P.,Andis, Sherri L.,Schoepp, Darryle D.
, p. 3099 - 3102 (2007/10/03)
The major excitatory neurotransmitter in the Central Nervous System is L-glutamic acid. As a result much attention has been given to the discovery of selective modulators of both the ionotropic glutamate receptors (iGluRs) and the metabotropic glutamate receptors (mGluRs). In this study we describe a novel class of subtype selective allosteric potentiators of the mGlu2 receptor. An active compound N-(4-phenoxyphenyl)-N-(3-pyridinylmethyl)ethanesulfonamide, LY181837, was identified in the course of compound screening. The synthesis of two series of analogs examined the structural requirements of the diaryl region of this compound. This SAR study also resulted in compounds with an increase in potency of over 100-fold where the most potent compound reported has EC 50=14nM.
