1382481-79-9Relevant articles and documents
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu 5 PAM
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)
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.