Potent and selective negative allosteric modulator of mGlu1 (IC50 = 99 nM). Exhibits >100-fold selectivity for mGlu1 over mGlu2-8 and 68 other GPCRs, ion channels, kinases and transporters. Brain penetrant.
Lovell et al (2013) N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg.Med.Chem.Lett. 23 3713 PMID:23727046