Positive allosteric modulator of mGlu5
= 16 nM; Ki
= 195 nM). Selective for mGlu5
; displays no significant activity at mGlu1
receptors. Exhibits antipsychotic-like activity in a rodent model. Also reduces spontaneous spike and wave discharges without affecting motor behaviour in a rat model of absence epilepsy.
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Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity.
Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats.
D'Amore et al.