Luzindole (N-0774) is a selective melatonin receptor antagonist which preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity[1][2][3].
Luzindole, identified as N-0774, acts as a melatonin receptor blocker with a higher affinity for MT2 (Mel1b) receptors compared to MT1 (Mel1a), demonstrated by Ki values of 10.2 nM for MT2 and 158 nM for MT1. It has been found to inhibit the progression of experimental autoimmune encephalomyelitis (EAE) and display properties akin to antidepressants[1][2][3]. Additionally, Luzindole at concentrations ranging from 5-10 μg/ml effectively hinders the antigen-specific growth of the MBP-responsive LV-4 T cell line[1].
Luzindole 动物研究
Animal study
Administering Luzindole at a dose of 30 mg/kg intraperitoneally from day 0 to day 5 has been shown to suppress experimental autoimmune encephalomyelitis[2]. Luzindole administered at 30 mg/kg intraperitoneally is observed to decrease immobility time in a dose-responsive manner, with a more significant effect at midnight, showing a 60% reduction, compared to a 39% reduction at noon. The peak impact of luzindole occurs at 60 minutes. However, the anti-immobility influence of luzindole at 10 mg/kg is counteracted by melatonin at 30 mg/kg. In albino ND/4 mice or C57BL/6J mice, which lack melatonin production, luzindole at 30 mg/kg does not alter immobility times at either noon or midnight[3].
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