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首页 / 抑制剂/激动剂 / 神经信号通路 / MT Receptor / Luzindole

Luzindole {[allProObj[0].p_purity_real_show]}

货号：A192769 同义名： N-0774 Ambeed 开学季，买赠积分，赢豪礼

Luzindole (N-0774) is a selective melatonin receptor antagonist which 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].

Luzindole 化学结构 CAS号：117946-91-5
Luzindole 化学结构
CAS号：117946-91-5
Luzindole 3D分子结构
CAS号：117946-91-5
Luzindole 化学结构 CAS号：117946-91-5
Luzindole 3D分子结构 CAS号：117946-91-5
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Luzindole 纯度/质量文件 产品仅供科研

货号：A192769 标准纯度： {[allProObj[0].p_purity_real_show]}
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Luzindole 生物活性

描述 Luzindole, identified as N-0774, acts as a melatonin receptor blocker with a higher affinity for MT2 (Mel1b) receptors compared to MT1 (Mel1a), demonstrated by Ki values of 10.2 nM for MT2 and 158 nM for MT1. It has been found to inhibit the progression of experimental autoimmune encephalomyelitis (EAE) and display properties akin to antidepressants[1][2][3]. Additionally, Luzindole at concentrations ranging from 5-10 μg/ml effectively hinders the antigen-specific growth of the MBP-responsive LV-4 T cell line[1].

Luzindole 动物研究

Animal study Administering Luzindole at a dose of 30 mg/kg intraperitoneally from day 0 to day 5 has been shown to suppress experimental autoimmune encephalomyelitis[2]. Luzindole administered at 30 mg/kg intraperitoneally is observed to decrease immobility time in a dose-responsive manner, with a more significant effect at midnight, showing a 60% reduction, compared to a 39% reduction at noon. The peak impact of luzindole occurs at 60 minutes. However, the anti-immobility influence of luzindole at 10 mg/kg is counteracted by melatonin at 30 mg/kg. In albino ND/4 mice or C57BL/6J mice, which lack melatonin production, luzindole at 30 mg/kg does not alter immobility times at either noon or midnight[3].

Luzindole 参考文献

[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 Ph

[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.

Luzindole 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.10mL

3.42mL

1.71mL

34.20mL

6.84mL

3.42mL

Luzindole 技术信息

CAS号117946-91-5
分子式C19H20N2O
分子量 292.375
别名 N-0774
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(359.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Luzindole | 117946-91-5 | N-0774 | N0774 | N 0774 | Melatonin Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Melatonin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Luzindole 纯度/质量文件 | Luzindole 生物活性 | Luzindole 参考文献 | Luzindole 实验方案 | Luzindole 技术信息

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