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雷美替胺 /Ramelteon {[allProObj[0].p_purity_real_show]}

货号:A428570 同义名: TAK-375

Ramelteon is a synthetic melatonin analogue working by binding to and activating melatonin receptors 1 and 2.

Ramelteon 化学结构 CAS号:196597-26-9
Ramelteon 化学结构
CAS号:196597-26-9
Ramelteon 3D分子结构
CAS号:196597-26-9
Ramelteon 化学结构 CAS号:196597-26-9
Ramelteon 3D分子结构 CAS号:196597-26-9
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Ramelteon 纯度/质量文件 产品仅供科研

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Ramelteon 生物活性

描述 Ramelteon, a potent and highly selective MT1/MT2 receptor agonist with Ki values of 14 and 112 pM respectively, is orally active and has potential for insomnia research. It consistently lowers the time it takes to fall asleep over prolonged use without causing any residual effects the next morning, or symptoms of rebound insomnia or withdrawal after stopping[1].[2].
体内研究

Ramelteon (administered orally; 0.1 and 1 mg/kg) effectively speeds up the adjustment of activity rhythms to new light-dark cycles in running wheel tests[3].

Ramelteon (administered orally; 3, 10, and 30 mg/kg) does not impair learning or memory as evidenced by performance in water maze tasks and the delayed match to position tasks in rats, suggesting no abuse potential for MT1/MT2 receptor agonists[3].

Ramelteon (administered orally at doses of 0.0001, 0.001, 0.01, and 0.1 mg/kg every 8 hours) markedly reduces wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, enhances slow-wave sleep at the same doses, and boosts rapid eye movement sleep at 0.1 mg/kg[4].

Ramelteon 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00642694 - Terminated(Enrollment disconti... 展开 >>nued based on mutually agreed upon decision by PI and funding sponsor) 收起 << - -
NCT02969343 Central Line-Associated Bloods... 展开 >>tream Infection (CLABSI) Venous Thromboembolism Patient Fall Catheter-Associated Infection Severe Hypoglycemia Opioid-Related Severe Adverse Drug Event Hospital Acquired Pressure Ulcer Adverse Drug Event Severe Hospital Acquired Delerium Rapid Response Related to Arrhythmia 收起 << Not Applicable Recruiting September 2018 United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Alexandra C Businger    617-732-7063    abusinger@partners.org    Contact: Patricia Dykes, RN PhD    617-732-8925    pdykes@partners.org    Principal Investigator: David W Bates, MD MSc 收起 <<
NCT00893269 Marijuana Dependence Phase 1 Completed - United States, Maryland ... 展开 >> Johns Hopkins University Baltimore, Maryland, United States, 21224 收起 <<

Ramelteon 参考文献

[1]Kato K, et al. Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005;48(2):301-310.

[2]Mayer G, et al. Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic primary insomnia. Sleep. 2009;32(3):351-360.

[3]Hirai K, et al. Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats. J Biol Rhythms. 2005;20(1):27-37.

[4]Miyamoto M, et al. The sleep-promoting action of ramelteon (TAK-375) in freely moving cats. Sleep. 2004;27(7):1319-1325.

Ramelteon 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.28mL

3.86mL

1.93mL

38.56mL

7.71mL

3.86mL

Ramelteon 技术信息

CAS号196597-26-9
分子式C16H21NO2
分子量 259.343
别名 TAK-375
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 50 mg/mL(192.79 mM),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

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

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