Luzindole
- N-Acetyl-2-benzyltryptamine; N-[2-[2-(Phenylmethyl)-1H-indol-3-yl]ethyl]acetamide
货号-规格 | 货期 | 价格 | 数量 |
abs819807-5mg | 4周 | ¥945.00 | - + |
abs819807-25mg | 4周 | ¥3209.00 | - + |

产品描述 | ||
描述 | Luzindole is a melatonin receptor antagonist, with a 25-fold higher affinity for the MEL-1B-R over the MEL-1A-R receptor subtype. Melatonin is a hormone produced endogenously from serotonin (5-HT), and melatonin interaction at the MEL-1B-R receptor is thought to represent a chemical underpinning for circadian rhythm and the sleep-wake cycle. Luzindole MEL-1B-R antagonism is described to modulate functions of melatonin signaling and the relationship between melatonin regulation and neurotransmission. Luzindole blocks melatonin-mediated inhibition of forskolin-stimulated cyclic AMP production in CHO cells. At 1μM Luzindole antagonizes the melatonin-elicited inhibition of calcium-dependent dopamine release, and at higher concentrations (from 1μM to 10μM) affects the response of this dopamine release mechanism to melatonin concentrations (shifts the dose-response curve). Melatonin activation of the MEL-1B-R receptor advances the circadian rhythm, and antagonism by Luzindole shows a similar shift in the dose-response curve for the response of biological timing to melatonin concentration, providing evidence that the MEL-1B-R receptor indeed represents a chemical foundation for the circadian timing system. Luzindole significantly antagonizes melatonin-mediated antinociception, suggesting that MEL-1B-R plays a further role as a mediator of melatonin modulation of pain signaling. | |
纯度 | ≥98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | N-Acetyl-2-benzyltryptamine; N-[2-[2-(Phenylmethyl)-1H-indol-3-yl]ethyl]acetamide | |
外观 | White to off-white crystalline solid | |
熔点 | 216.19° C (Predicted) | |
折射率 | n20D 1.63 (Predicted) | |
IC50 | melatonin-induced pigment aggregation : IC50 = 2.10 µM (frog); melatonin of Xenopus melanophores: IC50 = 2.46 µM (frog) | |
Ki 数据 | MEL-1B-R: Ki= 44.7 nM (human); MEL-1A-R: Ki= 603 nM (human); Melatonin receptor: Ki= 1606 nM (Gallus gallus) | |
可溶性/溶解性 | DMSO : 250 mg/mL (855.08 mM; Need ultrasonic) | |
生物活性 | ||
In vitro(体外研究) | Luzindole (N-0774) (5-10 μg/ml) inhibits antigen-specific proliferation of the MBP-reactive LV-4 T cell line. | |
In vivo(体内研究) | Luzindole (N-0774) (30 mg/kg; i.p.; days 0-5) suppresses experimental autoimmune encephalomyelitis. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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