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LY379268

CAS No. : 191471-52-0

MCE 站：LY379268

产品活性：LY379268 是一种有效、选择性和可透过血脑屏障的 mGlu2/3R 激动剂，EC₅₀ 值为 2.69 nM (mGlu2) 和 4.48 nM (mGlu3)。LY379268 对人 mGlu 1a、4a、5a 或 7a 受体没有活性。LY379268 具有抗氧化和神经保护作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: Treatment of 9-weeks (9w) astrocytes with LY379268 (0.1 μM; 24-48 hours) results in an increase in mGlu3R and Nrf2 protein levels and SOD activity, and decreases mitochondrial ROS levels and apoptosis. mGlu3R activation in aged astrocytes also preventS hippocampal neuronal death induced by Aβ1-42 in co-culture assays. Activation of mGlu3R in aged astrocytes haS an anti-oxidant effect and protected hippocampal neurons against Aβ-induced neurotoxicity.

In Vivo: For LY379268, when a 3?mg/kg dose is given prior to an intraplantar injection of carrageenan, the inflammatory hyperalgesia that developed is significantly delayed, without affecting the inflammation of the paw.
In a model of mouse tail withdrawal to warm water, LY379268 (12?mg/kg; i.p.), given before a subcutaneous tail injection of capsaicin, reduces the subsequent neurogenic hyperalgesia.LY354740 prevents release of glutamate in the striatum in freely moving rats and to attenuate morphine withdrawal-associated activation of locus coeruleus neurones, thought to be caused by an increased release of glutamate.

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