Luzindole,117946-91-5

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Luzindole

CAS No. : 117946-91-5

MCE 国际站：Luzindole

产品活性：Luzindole (N-0774) 是一种选择性褪黑素受体 (melatonin receptor) 拮抗剂。Luzindole 优先靶向 MT2 (Mel_1b)，对于人 MT2 和 MT1 的 K_i 值分别为 10.2 和 158 nM。Luzindole 抑制实验性自身免疫性脑脊髓炎，并发挥抗抑郁样活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Melatonin Receptor

In Vitro: Luzindole (N-0774) (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line.

In Vivo: Luzindole (N-0774) (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis.
Luzindole (N-0774) (30 mg/kg i.p.) reduces the time of immobility in a dose-dependent manner, the effect being more pronounced at midnight (60% reduction) than at noon (39% reduction). The effect of luzindole is time-dependent, showing a maximal effect at 60 min. The anti-immobility effect of luzindole (10 mg/kg i.p.) is prevented by the administration of melatonin (30 mg/kg i.p.). Luzindole (30 mg/kg i.p.) did not modify the time of immobility either at noon or midnight in the albino ND/4 mouse, or in the C57BL/6J mouse, which does not produce melatonin.

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