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| 品牌 | absin | CAS | 196597-26-9 |
|---|---|---|---|
| 分子式 | C16H21NO2 | 纯度 | ＞98% |
| 分子量 | 259.35 | 货号 | abs47027708 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | used for insomnia | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Ramelteon 196597-26-9
| 产品描述 | |
| 描述 | Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse. |
| 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 | 雷美替胺；TAK-375 |
| 外观 | 白色或类白色粉末 |
| 可溶性/溶解性 | DMSO : 49 mg/mL (188.9 mM) Ethanol : 49 mg/mL (188.9 mM) |
| 生物活性 | |
| 靶点 | MT1 receptor ,MT receptor (chicken) ,MT2 receptor |
| In vitro(体外研究) | Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. Ramelteon has high affinity with recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. Ramelteon inhibits Xenopus laevis melanophore pigment granule aggregation with pEC50 of 11.48. Ramelteon (1 nM) increases ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells but also in cerebellar granule cells expressing only one of the two melatonin receptors. 4P-PDOT blocks the stimulatory action of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, while luzindole attenuates the action of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon (100 μM) induces any pigment dispersion while melatonin completely disperses aggregated melanophores at 10 μM. |
| In vivo(体内研究) | Ramelteon (10 mg/kg, i/p) significantly reduces NREM sleep latency in rat and also produces a short-lasting increase in nonrapid eye movement (NREM) sleep duration, but the NREM power spectrum is unaltered. Ramelteon (0.1 mg/kg and 1 mg/kg, p.o.) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle in rats without affecting learning or memory. Ramelteon (0.03 mg/kg and 0.3 mg/kg, p.o.) significantly shortens latency to sleep onset and significantly increases total duration of sleep in freely moving monkeys without affecting the general behavior of the monkeys. |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | Neuroscience CancerTumor biomarkers NeuroscienceEndocrine system Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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