TAK-375 拉米替隆;雷美爾通;瑞美替胺 Ramelteon
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- 型號 TAK-375
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- 更新時間 2019/7/4 16:43:18
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| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL；2 mg；5 mg；10 mg；50 mg；100 m |
|---|---|---|---|
| 貨號 | HY-A0014 | 應(yīng)用領(lǐng)域 | 生物產(chǎn)業(yè) |
Ramelteon
產(chǎn)品活性：Ramelteon是高效選擇性的melatonin受體激動劑，結(jié)合人melatonin1和melatonin2受體的Ki值分別為14 和112 pM。
研究領(lǐng)域：GPCR/G Protein | Neuronal Signaling
作用靶點(diǎn)：Melatonin Receptor
In Vitro: Ramelteon shows very high affinity for human melatonin1 and melatonin2 receptors (expressed in CHO cells), and chick forebrain melatonin receptors (consisting of melatonin1 and melatonin2 receptors) with Ki values of 14.0, 112, and 23.1 pM, respectively. The affinity of ramelteon for hamster brain melatonin3 binding sites is extremely weak (Ki: 2.65 μM) compared to melatonin's affinity for the melatonin3 binding site Ki: 24.1 nM). In addition, ramelteon shows no measurable affinity for a large number of ligand binding sites (including benzodiazepine receptors, dopamine receptors, opiate receptors, ion channels, and transporters) and no effect on the activity of various enzymes. Ramelteon inhibits forskolin-stimulated cAMP production in the CHO cells that express the human melatonin1 and melatonin2 receptors.
In Vivo: Ramelteon 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 in freely moving cats. Ramelteon is associated with reduced subjective sleep latency and improved sleep quality. Ramelteon is associated with improvement in latency to persistent sleep, sleep efficiency , and total sleep time. Ramelteon (10 mg/kg, i/p), administered close to the mid-point of the dark phase of the L:D cycle, significantly reduces NREM sleep latency (time from injection to the appearance of NREM sleep). Ramelteon also produces a short-lasting increase in NREM sleep duration, but the NREM power spectrum is unaltered.
相關(guān)產(chǎn)品：FDA-Approved Drug Library Plus | Drug Repurposing Compound Library | FDA-Approved Drug Library Mini | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | CNS-Penetrant Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library Plus | Bioactive Compound Library Plus | Melatonin | Tasimelteon | Ramelteon metabolite M-II
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