1174047-14-3Relevant articles and documents
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype
Rodriguez, Alice L.,Williams, Richard,Zhou, Ya,Lindsley, Stacey R.,Le, Uyen,Grier, Mark D.,David Weaver,Jeffrey Conn,Lindsley, Craig W.
scheme or table, p. 3209 - 3213 (2010/03/31)
This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and the first example of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold.
