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LY3020371 hydrochloride

CAS No. : 1377615-44-5

MCE 国际站：LY3020371 hydrochloride

产品活性：LY3020371 hydrochloride 是一种有效的选择性代谢型谷氨酸 2/3 受体 (mGlu2/3) 拮抗剂，K_i 值分别为 5.3 nM 和 2.5 nM。LY3020371 hydrochloride 有效阻断 cAMP 形成，IC₅₀ 值为 16.2 nM。LY3020371 hydrochloride 在体内具有抗抑郁样特性。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

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).
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).
LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca²⁺ oscillations (IC₅₀=34 nM) and in an intact hippocampal slice preparation (IC₅₀=46 nM).

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.

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