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Overview
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Background
Luzindole is a melatonin receptor antagonist that preferentially targets MT2 over MT1. Luzindole inhibits experimental autoimmune encephalomyelitis and exerts antidepressant-like activity[1-3].
Luzindole (30 mg/kg i.p.) reduces the immobile time in a dose-dependent manner, reducing midnight by 60% and noon by 39%. Luzindole shows the greatest effect at 60 minutes. In albinism ND/4 mice or C57BL/6J mice that do not produce melatonin, Luzindole (30 mg/kg i.p.) does not change the immobile time at noon or midnight[3].[1]. Dubocovich M L, et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch Pharmacol, 1997, 355(3): 365-75.
[2]. Constantinescu C S, et al. Luzindole, a melatonin receptor antagonist, suppresses experimental autoimmune encephalomyelitis. Pathobiology, 1997, 65(4): 190-4.
[3]. Dubocovich M L Antidepressant-like activity of the melatonin receptor antagonist, luzindole (N-0774), in the mouse behavioral despair test. Eur J Pharmacol, 1990, 182(2): 313-25.
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