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Ramelteon metabolite M-II  

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包装规格：5mg 10mg in glass bottle
产品描述：基本信息 产品编号： R10498  产品名称： Ramelteon metabolite M-II CAS: 896736-21-3   储存条件 粉末 -20℃ 四年 分子式： C16H21NO3 溶于液体 -80℃ 二年 分子量： 275.34     化学名：  2-hydroxy-N-[2-[(8S)-2,6,7,8-tetrahydro-1H-cyclopenta[e][1]benzofuran-8-yl]ethyl]propanamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。   生物活性 产品描述 雷美替胺 (Ramelteon) 的主要代谢物，其对人褪黑素受体 1和2 的 IC50 值分别为 208pM 和 1470pM。雷美替胺是褪黑素受体 (melatonin) 的选择性激动剂。 靶点 Melatonin Receptor   体外研究 The affinity of Ramelteon metabolite M-II (M-II) for MT1 receptors is 10-and 2.5-fold lower than that of ramelteon and melatonin,respectively.Likewise, the affinity of M-II for MT2 receptors is approximately 5-and 1.5-fold lower than that of ramelteon and melatonin,respectively.Ramelteon metabolite M-II exhibits no affinity for quinone reductase 2 at concentrations up to 10μM.Moreover,the selectivity of Ramelteon metabolite M-II for melatonin receptors relative to 215 targets including other receptors,transporters,ion channels and enzymes is investigated.Ramelteon metabolite M-II shows no significant affinities and activities for the other targets,except for the 5-HT2B receptor,for which the Ki value was 1.75±0.23μM.The potency of Ramelteon metabolite M-II for MT1 receptors is approximately 17-and 4.3-fold lower than that of ramelteon and melatonin,respectively.Similarly,the potency of Ramelteon metabolite M-II for MT2 receptors is approximately 28- and 1.6-fold lower than that of ramelteon and melatonin,respectively. 体内研究 Ramelteon metabolite M-II (1mg/kg) significantly increases NREM sleep (F1,7=96.3,p<0.01) and significantly decreases wakefulness (F1,7=56.7,p<0.01).Moreover,a lower dose of M-II (0.1mg/kg) yield similar results (NREM, F1,7=121.9,p<0.01;wakefulness,F1,7=87.0,p<0.01),and decreased wakefulness is sustained for 6h after the administration of either dose.After the administration of 0.01mg/kg Ramelteon metabolite M-II,only NREM sleep is significantly increased (F1,7=10.5,p< 0.05).No significant differences in REM sleep are observed after the administration of M-II at any of the doses tested in this study.   推荐实验方法(仅供参考) 动物实验:   Cats Eight adult cats weighing 2.4-5.9kg are used in each study.The cats are housed individually in rooms maintained at 22-26℃ with a 12-h light-dark cycle (lights on at 7.00 a.m.),fed once daily (9.00 a.m.) and given water ad libitum.The cats are anesthetized, and electrodes are surgically implanted for electroencephalogram (EEG), electromyogram (EMG) and electrooculogram (EOG) monitoring. After a recovery period of at least 7 days,the cats are well accustomed to the test chamber (65×35×45 cm).Ramelteon metabolite M-II is orally administered at 0.1mL/kg to each cat using gelatin capsules.The effects of M-II on sleep are compared with those of the vehicle using a crossover design. The interval between trials is >6 days.The cats are given Ramelteon metabolite M-II (0.001,0.01,0.1 or 1mg/kg) or vehicle between 9.55 and 10.00 a.m.Immediately after the administration,EEG,EOG and EMG recordings are started sequentially and lasted 8h.The durations of sleep stages are measured after the administration of vehicle or M-II and are presented as mean percentages of time spent in each stage at each 2-hour period after administration.
保存条件：-20℃

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