2​ Biological Activity LY404039 is a selective metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3 agonist with Ki of 149 and 92nM for mGlu2 and mGlu3, respectively.Functional activity of LY404039 at group II and group III mGlu receptors is measured by the inhibition of forskolin-stimulated cAMP formation. It is nanomolar potent agonists at human mGlu2 and mGlu3 receptors, as indicated by the inhibition of forskolin-stimulated cAMP formation (LY404039: mGlu2, EC50 =23 nM; mGlu3, EC50 = 48 nM). It suppressed the frequency of 5-HT-induced EPSCs with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM. Intraperitoneal administration of LY404039 (10 mg/kg) to wild-type mice significantly inhibited increases evoked by PCP (7.5 mg/kg) in ambulations. It produced a dose-dependent reduction of increases evoked by AMP (5 mg/kg) in ambulations. [1][2][3] 3​ References: [1] Rorick-Kehn LM et al. J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. [2] Fell MJ et al. J Pharmacol Exp Ther. 2008 Jul;326(1):209-17. [3] http://en.wikipedia.org/wiki/LY-404,039 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.