LY3020371 hydrochloride

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor ( mGlu2/3 ) antagonist with K i of 5.3 and 2.5 nM, potently blocks cAMP formation with IC 50 of 16.2 nM LY3020371 hydrochloride exerts an antidepressant-like signature in vivo . In Vitro LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [ 3 H]-459477 with high affinity (hmGlu2 K i =5.26 nM; hmGlu3 K i =2.50 nM). LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC 50 =16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC 50 =6.21 nM). LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca 2+ oscillations (IC 50 =34 nM) and in an intact hippocampal slice preparation (IC 50 =46 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo LY3020371 hydrochloride (LY3020371.HCl) (Intravenous injection; 3-15 mg/kg) in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors . LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10 mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:mGluR2 5.3 nM (Ki) mGluR3 2.5 nM (Ki)

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