CAS NO: | 896736-21-3 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
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. |