Ramelteon

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ramelteon 是第一种新型睡眠化合物，可选择性地与视交叉上核 (SCN) 中的褪黑激素受体结合。

Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse. (In Vivo):Ramelteon (p.o.; 0.1 and 1 mg/kg) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle.Ramelteon (p.o.; 3, 10, and 30 mg/kg) does not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential.Ramelteon (0.0001, 0.001, 0.01, and 0.1 mg/kg; p.o.; 8 hours) significantly decreases wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increases slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increases rapid eye movement sleep at a dose of 0.1 mg/kg.

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Ramelteon (p.o.; 0.1 and 1 mg/kg) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle.Ramelteon (p.o.; 3, 10, and 30 mg/kg) does not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential.Ramelteon (0.0001, 0.001, 0.01, and 0.1 mg/kg; p.o.; 8 hours) significantly decreases wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increases slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increases rapid eye movement sleep at a dose of 0.1 mg/kg. Animal Model:Male Wistar or Fischer 344 (F344) rats Dosage:0.1 and 1 mg/kg; 3, 10, and 30 mg/kg Administration:p.o.Result:Accelerated reentrainment of running wheel activity rhythm to the new lightdark cycle. Ramelteon did not affect learning or memory in rats tested by the water maze task and the delayed match to position task, implying that MT1/MT2 receptor agonists have no abuse potential.Animal Model:Adult cats (2.5-6.1 kg) Dosage:0.0001, 0.001, 0.01, and 0.1 mg/kg Administration:p.o.; 8 hours Result:Significantly decreased wakefulness at doses of 0.001, 0.01, and 0.1 mg/kg, increased slow-wave sleep at doses of 0.001, 0.01, and 0.1 mg/kg, and increased rapid eye movement sleep at a dose of 0.1 mg/kg.

TAK-375

Metabolic Enzyme/Protease

MMP

MT receptor (chicken)| MT1 receptor| MT2 receptor

Neurological Disease

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196597-26-9

259.35

C16H21NO2

>98% (HPLC)

Ethanol: 52 mg/mL (200.5 mM); DMSO: 52 mg/mL (200.5 mM)

CCC(=O)NCC[C@@H]1CCC2=C1C3=C(C=C2)OCC3

(S)-N-(2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl)propionamide

(-20℃)

With Ice Pack

≥ 2 years