LY2812223 is highly potent, functionally selective mGlu2 receptor agonist with EC50 of 13.6 nM in GTPγS functional binding assay.
LY2812223 displays little to no affinity for mGlu1, mGlu4, mGlu5 or mGlu7 receptors.
LY2812223 fully displaces the mGlu2/3 agonist radioligand [3H]LY459477 with Ki of 118 nM, inhibits forskolin-stimulated cAMP with EC50 of 16.1 nM.
LY2812223 displays near maximal agonist responses at the mGlu2 receptor across all assay formats, while shows no functional agonist activity at the mGlu3 receptor except in the cAMP assay.
