Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu 5 PAM
Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) with 15-fold selectivity versus mGlu2. The mGlu3 NAM was discovered via a 'molecular switch' from a closely related, potent mGlu5 positive allosteric modulator (PAM), VU0092273. This NAM (VU0463597, ML289) displays an IC 50 value of 0.66 μM and is inactive against mGlu5.
Sheffler, Douglas J.,Wenthur, Cody J.,Bruner, Joshua A.,Carrington, Sheridan J.S.,Vinson, Paige N.,Gogi, Kiran K.,Blobaum, Anna L.,Morrison, Ryan D.,Vamos, Mitchell,Cosford, Nicholas D.P.,Stauffer, Shaun R.,Scott Daniels,Niswender, Colleen M.,Jeffrey Conn,Lindsley, Craig W.
p. 3921 - 3925
(2012/07/14)
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