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Ramelteon metabolite M-II
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ramelteon metabolite M-II图片
CAS NO:896736-21-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Ramelteon metabolite M-II 是雷美替胺 (Ramelteon) 的主要代谢物,其对人褪黑素受体 1 和 2 的 IC50值分别为 208 pM 和 1470 pM。雷美替胺是褪黑素受体 (melatonin) 的选择性激动剂。
生物活性

Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1or MT2). Ramelteon is a selective melatonin agonist.

体外研究
(In Vitro)

The affinity of Ramelteon metabolite M-II (M-II) for MT1receptors is 10- and 2.5-fold lower than that of ramelteon and melatonin, respectively. Likewise, the affinity of M-II for MT2receptors 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 10 μM. 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-HT2Breceptor, for which the Kivalue was 1.75±0.23 μM. The potency of Ramelteon metabolite M-II for MT1receptors is approximately 17- and 4.3-fold lower than that of ramelteon and melatonin, respectively. Similarly, the potency of Ramelteon metabolite M-II for MT2receptors is approximately 28- and 1.6-fold lower than that of ramelteon and melatonin, respectively[1].

体内研究
(In Vivo)

Ramelteon metabolite M-II (1 mg/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 (0.1 mg/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 6 h after the administration of either dose. After the administration of 0.01 mg/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[1].

分子量

275.34

Formula

C16H21NO3

CAS 号

896736-21-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.