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Luzindole (N-0774) is a selective competitive melatonin MT1/MT2 antagonist with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole inhibits experimental autoimmune encephalomyelitis and exerts antidepressant-like activity. Luzindole (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line.
In Twenty-three- to 12-week-old (SJL X PL/J ) F1 mice, Luzindole (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis.
| Molecular Weight | 292.38 |
| Formula | C19H20N2O |
| CAS Number | 117946-91-5 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Melatonin Receptor Products |
|---|
| Melatonin
Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. |
| Agomelatine
Agomelatine is a metabolically stable analog of melatonin that displays agonist activity for MT1 and MT2 binding with nanomolar affinity. Agomelatine is also a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively. |
| Ramelteon (TAK-375)
Ramelteon (TAK-375) is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively. |
| 2-Phenylmelatonin
2-Phenylmelatonin is a potent melatonin agonist. |
| Tasimelteon
Tasimelteon (BMS-214778) is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep–wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light–dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep–wake schedules. |
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