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Ramelteon metabolite M-II

Catalog No. T12689 CAS 896736-21-3

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.

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Ramelteon metabolite M-II Chemical Structure

Ramelteon metabolite M-II, CAS 896736-21-3

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1 mg	35 days	$ 233.00
5 mg	35 days	$ 688.00
10 mg	35 days	$ 1,250.00

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Biological Description

Chemical Properties

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Description	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.
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. 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.
In vivo	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.

Molecular Weight	275.34
Formula	C16H21NO3
CAS No.	896736-21-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Nishiyama K, et al. Pharmacological characterization of M-II, the major human metabolite of ramelteon. Pharmacology. 2014;93(3-4):197-201.

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Keywords

Ramelteon metabolite M-II 896736-21-3 Others Ramelteon metabolite MII Ramelteon metabolite M II inhibitor inhibit

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