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VU0360223 is a noncompetitive antagonist (negative allosteric modulator) of mGlu5 that demonstrates an IC50 value of 61 nM in a calcium mobilization assay and a Ki value of 477 nM in a radioligand binding assay.1 A 10 μM concentration of VU0360223 results in a near complete blockade of the glutamate response in cortical astrocytes.1 A 30 mg/kg dose of VU0360223 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.1
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