- Potent mGlu5 positive allosteric modulator (EC50 = 1.5 nM) and agonist (EC50 = 171 nM; maximum effect is 65% that of glutamate).
- Binds allosteric site with high affinity (Ki = 11.8 nM).
- Increases maximum response to glutamate by 30%.
- Exhibits bias towards signaling via IP1 and ERK1/2 over iCa2+ in HEK293 and neuronal cells, and activates Gs in HEK 293 cells.
- Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo.