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Bioorg Med Chem Lett. 2012 Feb 15;22(4):1575-8. doi: 10.1016/j.bmcl.2011.12.131. Epub 2012 Jan 3.

Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain.

Author information

1
Merck Research Laboratories, Kenilworth, NJ 07033-0539, USA. chadbennett3@yahoo.com

Abstract

A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.

PMID:
22266036
DOI:
10.1016/j.bmcl.2011.12.131
[Indexed for MEDLINE]

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