Format

Send to:

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem Lett. 2009 Jun 15;19(12):3209-13. doi: 10.1016/j.bmcl.2009.04.110. Epub 2009 May 3.

Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

Author information

  • 1Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

Abstract

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.

PMID:
19443219
[PubMed - indexed for MEDLINE]
PMCID:
PMC3177605
Free PMC Article
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science Icon for PubMed Central
    Loading ...
    Write to the Help Desk