AZD9272 is a potent, selective, highly CNS-penetrant and orally available mGluR5 negative allosteric modulator Kd of 2.8 nM.
AZD9272 does not elicit any agonist, antagonist or positive allosteric modulator on any of the other seven mGluR subtypes at 30 uM.
AZD9272 completely reverses the glutamate-stimulated phosphatidyl inositol hydrolysis in human mGluR5-GHEK cells with IC50 of 26 nM.
AZD9272 causes psychoactive effects selectively mediated by mGluR5 mechanisms in vivo,
