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    Ramelteon
    Ramelteon
    Information
    CAS No. 166597-26-9 Price
    Catalog No.CFN90021Purity>=98%
    Molecular Weight259.34Type of CompoundAlkaloids
    FormulaC13H21NO2Physical DescriptionWhite powder
    Download     COA    MSDS    SDFSimilar structuralComparison (Web)
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    Ramelteon Description
    Source:
    Biological Activity or Inhibitors: 1. Ramelteon significantly improves symptoms in patients with gastroesophageal reflux disease and significantly improves patients' sleep experience.
    2. Ramelteon could be a potential therapeutic drug, in adjunctive treatment of learning and memory deficits seen in patients with schizophrenia.
    3. Ramelteon is effective for the prevention of delirium, ramelteon administered nightly to elderly patients admitted for acute care may provide protection against delirium.
    4. Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for insomnia treatment, demonstrates no significant effects indicative of potential for abuse or motor and cognitive impairment at up to 20 times the recommended therapeutic dose.
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

    After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 3.8559 mL 19.2797 mL 38.5594 mL 77.1188 mL 96.3986 mL
    5 mM 0.7712 mL 3.8559 mL 7.7119 mL 15.4238 mL 19.2797 mL
    10 mM 0.3856 mL 1.928 mL 3.8559 mL 7.7119 mL 9.6399 mL
    50 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.5424 mL 1.928 mL
    100 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.7712 mL 0.964 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Ramelteon References Information
    Citation [1]

    Arch Gen Psychiatry. 2006 Oct;63(10):1149-57.

    Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects.[Pubmed: 17015817 ]
    Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for insomnia treatment. Most approved insomnia medications have potential for abuse and cause motor and cognitive impairment. OBJECTIVE: To evaluate the potential for abuse, subjective effects, and motor and cognitive-impairing effects of Ramelteon compared with triazolam, a classic benzodiazepine sedative-hypnotic drug. RESULTS: Compared with placebo, Ramelteon (16, 80, and 160 mg) showed no significant effect on any of the subjective effect measures, including those related to potential for abuse. In the pharmacological classification, 79% (11/14) of subjects identified the highest dose of Ramelteon as placebo. Similarly, compared with placebo, Ramelteon had no effect at any dose on any observer-rated or motor and cognitive performance measure. In contrast, triazolam showed dose-related effects on a wide range of subject-rated, observer-rated, and motor and cognitive performance measures, consistent with its profile as a sedative drug with abuse liability. CONCLUSION: Ramelteon demonstrated no significant effects indicative of potential for abuse or motor and cognitive impairment at up to 20 times the recommended therapeutic dose and may represent a useful alternative to existing insomnia medications.
    Citation [2]

    J Clin Gastroenterol. 2015 Apr 9.

    The Effect of Ramelteon on Heartburn Symptoms of Patients With Gastroesophageal Reflux Disease and Chronic Insomnia: A Pilot Study.[Pubmed: 25887111]
    BACKGROUND: There is a bidirectional relationship between gastroesophageal reflux disease (GERD) and sleep. It has been demonstrated that antireflux treatment can improve sleep quality in GERD patients with nighttime reflux. MATERIALS AND METHODS: Patients with heartburn and/or regurgitation ≥3 times/week and insomnia for ≥3 months were included. Patients were assessed at baseline with the demographic, GERD symptom assessment scale, Epworth sleepiness scale, Berlin sleep apnea, Pittsburgh sleep quality index, and the Insomnia severity index questionnaires. Subjects underwent an upper endoscopy followed by pH testing. Subsequently, subjects were randomized, in a double-blind, placebo-controlled trial, to receive either Ramelteon 8 mg or placebo before bedtime for 4 weeks. During the last week of treatment, subjects completed a daily GERD symptom and sleep diary and underwent actigraphy. RESULTS: Sixteen patients completed the study, 8 in each arm (mean age and M/F were 48.5 vs. 57.8 y, and 8/0 vs. 6/2, respectively). Patients who received Ramelteon demonstrated a statistically significant decrease in symptom score as compared with those who received placebo for daytime heartburn (-42% vs. -29%), nighttime heartburn (-42% vs. 78%), 24-hour heartburn (-42% vs. -3%), and 24-hour acid regurgitation (-26% vs. 19%) (all P<0.05). Insomnia severity index score was significantly reduced in patients receiving Ramelteon as compared with placebo (-46% vs. -5%, P<0.05). Ramelteon group also demonstrated a significant improvement in sleep efficiency and sleep latency, as compared with placebo, P<0.05). No significant adverse events were observed with Ramelteon. CONCLUSIONS: Ramelteon significantly improved symptoms in patients with GERD. In addition, Ramelteon significantly improved patients' sleep experience. Further studies are needed in the future (NCT01128582).
    Citation [3]

    Clin Psychopharmacol Neurosci. 2014 Dec;12(3):215-7.

    Effects of Add-on Ramelteon on Cognitive Impairment in Patients with Schizophrenia: An Open-label Pilot Trial.[Pubmed: 25598825]
    OBJECTIVE: This open-label study examined the effects of Ramelteon on cognitive functions in 10 outpatients with schizophrenia. METHODS: Ramelteon (8 mg/day) was administered to 10 patients with schizophrenia for six months. The verbal fluency test, Trail-Making Test, the Wisconsin Card Sorting Test, the Stroop Test, the Digit Span Distraction Test, Iowa Gambling Task, the Rey Auditory Verbal Learning Test were evaluated at baseline and 6 months after treatment with Ramelteon. RESULTS: Ramelteon improved significantly the scores of Rey Auditory Verbal Learning Test. Additionally, Ramelteon exerted improvements in the verbal fluency and Iowa Gambling Task in 4 patients. CONCLUSION: Ramelteon could be a potential therapeutic drug, in adjunctive treatment of learning and memory deficits seen in patients with schizophrenia.
    Citation [4]

    JAMA Psychiatry. 2014 Apr;71(4):397-403.

    Preventive effects of ramelteon on delirium: a randomized placebo-controlled trial.[Pubmed: 24554232]
    IMPORTANCE: No highly effective interventions to prevent delirium have been identified. OBJECTIVE: To examine whether Ramelteon, a melatonin agonist, is effective for the prevention of delirium. DESIGN, SETTING, AND PARTICIPANTS: A multicenter, rater-blinded, randomized placebo-controlled trial was performed in intensive care units and regular acute wards of 4 university hospitals and 1 general hospital. Eligible patients were 65 to 89 years old, newly admitted due to serious medical problems, and able to take medicine orally. Patients were excluded from the study if they had an expected stay or life expectancy of less than 48 hours. INTERVENTIONS: Sixty-seven patients were randomly assigned using the sealed envelope method to receive Ramelteon (8 mg/d; 33 patients) or placebo (34 patients) every night for 7 days. MAIN OUTCOMES AND MEASURES: Incidence of delirium, as defined by the Diagnostic and Statistical Manual of Mental Disorders (Fourth Edition). RESULTS: Ramelteon was associated with a lower risk of delirium (3% vs 32%; P = .003), with a relative risk of 0.09 (95% CI, 0.01-0.69). Even after risk factors were controlled for, Ramelteon was still associated with a lower incidence of delirium (P = .01; odds ratio, 0.07 [95% CI, 0.008-0.54]). The Kaplan-Meier estimates of time to development of delirium were 6.94 (95% CI, 6.82-7.06) days for Ramelteon and 5.74 (5.05-6.42) days for placebo. Comparison by log-rank test showed that the frequency of delirium was significantly lower in patients taking Ramelteon than in those taking placebo (χ(2) = 9.83; P = .002). CONCLUSIONS AND RELEVANCE: Ramelteon administered nightly to elderly patients admitted for acute care may provide protection against delirium. This finding supports a possible pathogenic role of melatonin neurotransmission in delirium.