Ramelteon metabolite M-II,8967

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Ramelteon metabolite M-II

CAS No. : 896736-21-3

MCE 国际站：Ramelteon metabolite M-II

产品活性：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。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Metabolic Enzyme/Protease

作用靶点：Melatonin Receptor  |  Drug Metabolite

In Vitro: 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 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-HT_2B receptor, for which the Ki value was 1.75±0.23 μM. 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.

In Vivo: Ramelteon metabolite M-II (1 mg/kg) significantly increases NREM sleep (F_1,7=96.3, p<0.01) and significantly decreases wakefulness (F_1,7=56.7, p<0.01). Moreover, a lower dose of M-II (0.1 mg/kg) yield similar results (NREM, F_1,7=121.9, p<0.01; wakefulness, F_1,7=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 (F_1,7=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.

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