1. GPCR/G Protein
    Neuronal Signaling
  2. Melatonin Receptor
  3. Luzindole

Luzindole (Synonyms: N-0774)

Cat. No.: HY-101254 Purity: 100.00%
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Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.

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Luzindole Chemical Structure

Luzindole Chemical Structure

CAS No. : 117946-91-5

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10 mM * 1 mL in DMSO USD 193 In-stock
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
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Description

Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity[1][2][3].

IC50 & Target

Ki :10.2 nM (human MT2), 158 nM (human MT1)[1]

In Vitro

Luzindole (N-0774) (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line[1].

In Vivo

Luzindole (N-0774) (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis[2].
Luzindole (N-0774) (30 mg/kg i.p.) reduces the time of immobility in a dose-dependent manner, the effect being more pronounced at midnight (60% reduction) than at noon (39% reduction). 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.). 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].

Animal Model: Twenty-three- to 12-week-old(SJL X PL/J ) F1 mice[2]
Dosage: 30 mg/kg
Administration: i.p.; days 0-5 (between 23: 00 and 1: 00 under conditions of minimal lighting)
Result: Effectively prevented experimental autoimmune encephalomyelitis.
Molecular Weight

292.37

Formula

C₁₉H₂₀N₂O

CAS No.

117946-91-5

SMILES

CC(NCCC1=C(CC2=CC=CC=C2)NC3=C1C=CC=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: 100.00%

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Keywords:

LuzindoleN-0774N0774N 0774Melatonin Receptorselectivepreferentiallyautoimmuneencephalomyelitisantidepressant-likesubtypeanti-immobilityInhibitorinhibitorinhibit

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