Ramelteon 是一种强效、高选择性和具有口服活性的MT1/MT2激动剂，Ki值分别为 14 和 112 pM。Ramelteon 具有研究失眠症的潜力。Ramelteon长期使用持续减少睡眠发作，停药后无翌日晨残留效应或反弹性失眠或戒断症状。
| 生物活性 | Ramelteon is a potent, highly selective, and orally active agonist ofMT1/MT2withKivalues of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2]. |
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体内研究
(In Vivo) | Ramelteon (p.o.; 0.1 and 1 mg/kg) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle[3].
Ramelteon (p.o.; 3, 10, and 30 mg/kg) does not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential[3].
Ramelteon (0.0001, 0.001, 0.01, and 0.1 mg/kg; p.o.; 8 hours) significantly decreases wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increases slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increases rapid eye movement sleep at a dose of 0.1 mg/kg[4].
| Animal Model: | Male Wistar or Fischer 344 (F344) rats[3] | | Dosage: | 0.1 and 1 mg/kg; 3, 10, and 30 mg/kg | | Administration: | p.o. | | Result: | Accelerated reentrainment of running wheel activity rhythm to the new lightdark cycle. Ramelteon did not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential. |
| Animal Model: | Adult cats (2.5-6.1 kg)[4] | | Dosage: | 0.0001, 0.001, 0.01, and 0.1 mg/kg | | Administration: | p.o.; 8 hours | | Result: | Significantly decreased wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increased slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increased rapid eye movement sleep at a dose of 0.1 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(192.80 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.8559 mL | 19.2797 mL | 38.5594 mL | | 5 mM | 0.7712 mL | 3.8559 mL | 7.7119 mL | | 10 mM | 0.3856 mL | 1.9280 mL | 3.8559 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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