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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)
100 mg电议
500 mg电议

产品介绍

产品描述

Ramelteon metabolite M-II is the major Ramelteon metabolite(human melatonin receptors (MT1 or MT2) with IC50s of 208 pM, 1470 pM). Ramelteon is an agonist of selective melatonin.

体外活性

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. The selectivity of M-II for melatonin receptors relative to 215 targets including other receptors, transporters, ion channels and enzymes is investigated. 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±0.23 μM. The potency of M-II for MT1 receptors is approximately 17- and 4.3-fold lower than that of ramelteon and melatonin, respectively. Similarly, the potency of M-II for MT2 receptors is approximately 28- and 1.6-fold lower than that of ramelteon and melatonin, respectively.

体内活性

Ramelteon metabolite M-II 1 mg/kg significantly increases NREM sleep and significantly decreases wakefulness. 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 M-II, only NREM sleep is significantly increased . No significant differences in REM sleep are observed after the administration of M-II at any of the doses tested in this study.

Cas No.

896736-21-3

分子式

C16H21NO3

分子量

275.34

别名

Ramelteon metabolite M-II

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years