LY3020371 is a potent and selective antagonist ofglutamate (mGlu) 2/3 receptor, withK_is of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression^[1][2].

LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [³H]-459477 with high affinity^[1].
LY3020371 (0.1 nM-100 μM) blocks DCG-IV-induced inhibition of forskolin-stimulated cAMP production in cells expressing recombinant human mGlu2 (IC₅₀=16.2 nM) and mGlu3 (IC₅₀=6.21 nM) receptors^[1].
LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation^[1].
LY3020371 (1-10000 nM) reverses LY379268-suppressed, K⁺-evoked glutamate release, with an IC₅₀of 86 nM^[1].
LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC₅₀of 33.9 nM^[1].

LY3020371 (0.3-3 mg/kg, a single i.v.) significantly increases the number of spontaneously active dopamine cells in the ventral tegmental area (VTA) of rats^[2].
LY3020371 (1-10 mg/kg, i.p. once a week for 5 weeks) dose dependently increases tissue oxygen in the anterior cingulate cortex (ACC) of rats^[2].
LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats^[2].
LY3020371 (1-30 mg/kg, a single i.v.) increases the cumulative wake time of rats in a dose- and time-dependent manner without rebound hypersomnolence^[2].
LY3020371 (0.1-10 mg/kg, a single i.v.) decrease the time rats are immobile in the forced-swim test in the rat forced-swim assay^[2].

359.35

C₁₅H₁₅F₂NO₅S

1377615-75-2

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