Drug intelligence / Profile preview

luzindole

Development stage
Preclinical
Lead developer
Boehringer
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Luzindole is a synthetic small molecule primarily utilized in scientific research as a selective melatonin receptor antagonist. It exhibits a higher affinity for the MT2 receptor (Mel1b) compared to the MT1 receptor (Mel1a), with reported Ki values of approximately 10.2 nM for human MT2 and 158 nM for human MT1, or 7.3 nM for MT2 and 179 nM for MT1, depending on the source. By blocking these receptors, luzindole interferes with the physiological actions of melatonin. Research indicates its involvement in disrupting circadian rhythms and demonstrating antidepressant-like effects in animal models. It has also been studied for its potential to suppress experimental autoimmune encephalomyelitis (EAE). While predominantly acting as an antagonist, some studies suggest it may also function as a partial agonist at MT2 for specific signaling pathways.

Other names
2-benzyl-N-acetyltryptamine
02

Targets

KCND2 (Transient outward potassium channel subunit Kv4.2)MTNR1A (MT1)MTNR1B (Melatonin Receptor 2)

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