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Bioorg Med Chem Lett. 2011 Dec 1;21(23):6955-9. doi: 10.1016/j.bmcl.2011.09.131. Epub 2011 Oct 8.

Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.

Author information

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

Abstract

Herein we report the discovery and SAR of a novel antagonist of metabotropic glutamate receptor 4 (mGlu(4)). The antagonist was discovered via a molecular switch from a closely related mGlu(4) positive allosteric modulator (PAM). This antagonist (VU0448383) displays an IC(50) value of 8.2±0.4 μM and inhibits an EC(80) glutamate response by 63.1±6.6%.

PMID:
22030026
PMCID:
PMC3319082
DOI:
10.1016/j.bmcl.2011.09.131
[Indexed for MEDLINE]
Free PMC Article

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