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LY3020371

CAS No. : 1377615-75-2

MCE 站：LY3020371

产品活性：LY3020371 是一种有效和选择性的谷氨酸受体 (mGluR2/3) 拮抗剂，对 hmGluR2 和 hmGluR3 的 K_i 值分别为 5.26 和 2.50 nM。LY3020371 可用于抑郁症的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [³H]-459477 with high affinity.
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.
LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation.
LY3020371 (1-10000 nM) reverses LY379268-suppressed, K⁺-evoked glutamate release, with an IC₅₀ of 86 nM.
LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC₅₀ of 33.9 nM.

In Vivo: 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.
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.
LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats.
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.
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.

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