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Luzindole

Catalog No. T15795   CAS 117946-91-5
Synonyms: N-0774

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.

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Luzindole Chemical Structure
Luzindole, CAS 117946-91-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 47.00
5 mg In stock $ 147.00
10 mg In stock $ 249.00
25 mg In stock $ 419.00
50 mg In stock $ 618.00
100 mg In stock $ 875.00
500 mg In stock $ 1,750.00
1 mL * 10 mM (in DMSO) In stock $ 158.00
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Purity: 98.96%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 MT2 receptor:10.2 nM(ki), MT1 receptor:158 nM(ki)
In vitro Luzindole (5-10 μg/ml) suppresses antigen-specific proliferation of the MBP-reactive LV-4 T cell line[1].
In vivo 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.).
Synonyms N-0774
Molecular Weight 292.37
Formula C19H20N2O
CAS No. 117946-91-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (342.03 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Dubocovich ML, 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 Mar;355(3):365-75. 2. Constantinescu CS, et al. Luzindole, a melatonin receptor antagonist, suppresses experimental autoimmune encephalomyelitis. Pathobiology. 1997;65(4):190-4. 3. Dubocovich ML Antidepressant-like activity of the melatonin receptor antagonist, luzindole (N-0774), in the mouse behavioral despair test. Eur J Pharmacol. 1990 Jul 3;182(2):313-25.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Inhibitor Library Membrane Protein-targeted Compound Library ReFRAME Related Library Bioactive Compound Library Histamine & Melatonin Receptor-Targeted Compound Library Antidepressant Compound Library Human Endogenous Metabolite Compound Library Plus Bioactive Compounds Library Max Neuronal Signaling Compound Library

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Keywords

Luzindole 117946-91-5 GPCR/G Protein Neuroscience Melatonin Receptor MT Receptor N0774 inhibit autoimmune anti-immobility subtype preferentially selective N 0774 Inhibitor encephalomyelitis antidepressant-like N-0774 inhibitor

 

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