1.
Bioorg Med Chem Lett
; 22(12): 3921-5, 2012 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22607673
RESUMO
Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu(3)) NAM probe (ML289) with 15-fold selectivity versus mGlu(2). The mGlu(3) NAM was discovered via a 'molecular switch' from a closely related, potent mGlu(5) positive allosteric modulator (PAM), VU0092273. This NAM (VU0463597, ML289) displays an IC(50) value of 0.66 µM and is inactive against mGlu(5).