Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole inhibits experimental autoimmune encephalomyelitis and exerts antidepressant-like activity. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively.

MT1 receptor:158 nM(ki), MT2 receptor:10.2 nM(ki)

Luzindole (5-10 μg/ml) suppresses antigen-specific proliferation of the MBP-reactive LV-4 T cell line[1].

Luzindole (30 mg/kg i.p.) decreases the time of immobility in a dose-dependent manner, the effect being more pronounced at midnight (60% reduction) than at noon (39% reduction). Luzindole (30 mg/kg; i.p.; days 0-5) inhibits experimental autoimmune encephalomyelitis[2]. 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[3]. 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.).