Ramelteon

Catalog No.S1259 Synonyms: TAK-375

Ramelteon Chemical Structure

Molecular Weight(MW): 259.34

Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.

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In DMSO USD 280 In stock
USD 110 In stock
USD 470 In stock
USD 997 In stock
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Cited by 4 Publications

3 Customer Reviews

  • (M) (Left) Cresyl violet and Luxol fast blue staining of ipsilateral corpus striatum on day 3 post-TBI. Scale bar = 50 µm. (Right) Bar graph shows that ramelteon did not increase the percentage of area with normal myelin in the Nrf2 KO mouse brain compared with that in the vehicle group. n = 6 mice/group. *P < 0.05 vs. sham group (one-way ANOVA followed by Bonferroni post hoc test). (N) (Left) Fluoro-Jade C staining of the perilesional cerebral cortex on day 3 post-TBI. Scale bar = 30 µm. (Right) Bar graph shows that ramelteon did not decrease the number of degenerating neurons in the perilesional region of the Nrf2 KO mice. n = 6 mice/group. *P < 0.05 vs. sham group (one-way ANOVA followed by Bonferroni post hoc test).

    Free Radic Biol Med, 2018, 131:345-355. Ramelteon purchased from Selleck.

    (A) CLSM images of Porphyromonas gingivalis biofilm formed in the presence of melatonin and ramelteon at sub-MIC concentrations. Biofilm-forming cells were stained using the Live/Dead Bacterial Viability Kit. Dead cells were stained red, whereas live bacteria were stained green. In the presence of 50 μg/mL or 25 μg/mL ramelteon, the areas of biofilm formation were narrower than that of vehicle controls. Bars = 50 μm.

    PLoS One, 2016, 11(11):e0166442.. Ramelteon purchased from Selleck.

  • Porphyromonas gingivalis were incubated in the presence of ramelteon (B). After crystal violet staining, absorbance at 550 nm was recorded. Data represent the mean ± SEM (n = 3) and differences between groups were assessed by ANOVA, *P < 0.05 versus vehicle control; **P < 0.01 versus vehicle control. three experiments.

    PLoS One, 2016, 11(11):e0166442. Ramelteon purchased from Selleck.

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Biological Activity

Description Ramelteon is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with Ki of 14 pM, 112 pM and 23.1 pM, respectively.
Features A tricyclic synthetic analog of melatonin.
Targets
MT1 receptor [1]
(Cell-free assay)
MT receptor (chicken) [1]
(Cell-free assay)
MT2 receptor [1]
(Cell-free assay)
14 pM(Ki) 23.1 pM(Ki) 112 pM(Ki)
In vitro

Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. [1] Ramelteon has high affinity with recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. Ramelteon inhibits Xenopus laevis melanophore pigment granule aggregation with pEC50 of 11.48. [2] Ramelteon (1 nM) increases ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells but also in cerebellar granule cells expressing only one of the two melatonin receptors. 4P-PDOT blocks the stimulatory action of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, while luzindole attenuates the action of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon (100 μM) induces any pigment dispersion while melatonin completely disperses aggregated melanophores at 10 μM. [3]

In vivo Ramelteon (10 mg/kg, i/p) significantly reduces NREM sleep latency in rat and also produces a short-lasting increase in nonrapid eye movement (NREM) sleep duration, but the NREM power spectrum is unaltered. [2] Ramelteon (0.1 mg/kg and 1 mg/kg, p.o.) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle in rats without affecting learning or memory. [4] Ramelteon (0.03 mg/kg and 0.3 mg/kg, p.o.) significantly shortens latency to sleep onset and significantly increases total duration of sleep in freely moving monkeys without affecting the general behavior of the monkeys. [5]

Protocol

Animal Research:[4]
+ Expand
  • Animal Models: estrogen-deficient ovariectomized (OVX) rats
  • Formulation: 0.5% methylcellulose solution
  • Dosages: 1 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 52 mg/mL (200.5 mM)
Ethanol 52 mg/mL (200.5 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 259.34
Formula

C16H21NO2

CAS No. 196597-26-9
Storage powder
in solvent
Synonyms TAK-375

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03165695 Not yet recruiting Delirium in Old Age Brigham and Women''s Hospital June 1 2019 Phase 4
NCT03165695 Not yet recruiting Delirium in Old Age Brigham and Women''s Hospital June 1 2019 Phase 4
NCT03461042 Recruiting Chronic Insomnia Translational Research Center for Medical Innovation Kobe Hyogo Japan|Yoyogi Sleep Disorder Clinic Foundation of Sleep and Health Science February 6 2018 Phase 4
NCT03461042 Recruiting Chronic Insomnia Translational Research Center for Medical Innovation Kobe Hyogo Japan|Yoyogi Sleep Disorder Clinic Foundation of Sleep and Health Science February 6 2018 Phase 4
NCT03265951 Recruiting Insomnia State University of New York at Buffalo|The VA Western New York Healthcare System January 1 2018 Phase 4
NCT03265951 Recruiting Insomnia State University of New York at Buffalo|The VA Western New York Healthcare System January 1 2018 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID