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 IC₅₀ of 16.2 nM^[1]. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo^[2]. IC50 & Target: Ki: 5.26 nM (hmGlu2); 2.50 nM (hmGlu3) LY3020371 hydrochloride^[1] In Vitro: LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [³H]-459477 with high affinity (hmGlu2 K_i=5.26 nM; hmGlu3 K_i=2.50 nM)^[1].
LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC₅₀=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC₅₀=6.21 nM)^[1].
LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca²⁺ oscillations (IC₅₀=34 nM) and in an intact hippocampal slice preparation (IC₅₀=46 nM)^[1].
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^[1].
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^[3].