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Luzindole

Catalog No. T15795 CAS 117946-91-5

Synonyms: N-0774, N-乙酰-2-苄基色胺

Luzindole 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, CAS 117946-91-5

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Purity: 98%

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Description	Luzindole 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, N-乙酰-2-苄基色胺
Molecular Weight	292.37
Formula	C19H20N2O
CAS No.	117946-91-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (342.03 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

Inhibitor Library Neuronal Signaling Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

ACH-000143 N-ACETYLTRYPTAMINE Tasimelteon Melatonin Luzindole Ramelteon Agomelatine 4-P-PDOT

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Keywords

Luzindole 117946-91-5 G蛋白偶联受体神经科学 Melatonin Receptor MT Receptor inhibit autoimmune anti-immobility subtype preferentially selective N-0774 Inhibitor encephalomyelitis N 0774 antidepressant-like N0774 inhibitor

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