331866-35-4Relevant academic research and scientific papers
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS
Zhou, Ya,Rodriguez, Alice L.,Williams, Richard,Weaver, C. David,Conn, P. Jeffrey,Lindsley, Craig W.
scheme or table, p. 6502 - 6506 (2010/05/17)
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 identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold.
