Catalog No.S1259 Synonyms: TAK-375

For research use only.

Ramelteon (TAK-375) 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.

Ramelteon Chemical Structure

CAS No. 196597-26-9

Selleck's Ramelteon has been cited by 7 Publications

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Biological Activity

Description Ramelteon (TAK-375) 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.
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 (from reference)

Animal Research:[4]
  • Animal Models: estrogen-deficient ovariectomized (OVX) rats
  • Dosages: 1 mg/kg
  • Administration: Orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 259.34


CAS No. 196597-26-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(=O)NCCC1CCC2=C1C3=C(C=C2)OCC3

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03931070 Completed Drug: Ramelteon|Drug: Placebo - Cap Delirium Rhode Island Hospital May 9 2019 Phase 4
NCT02560324 Completed Drug: Ramelteon|Drug: Placebo Tobacco Use Disorder University of Pennsylvania|National Institute on Drug Abuse (NIDA)|National Institutes of Health (NIH) September 2015 Phase 2
NCT02969343 Completed Behavioral: Patient Safety health information technology Central Line-Associated Bloodstream Infection (CLABSI)|Venous Thromboembolism|Patient Fall|Catheter-Associated Infection|Severe Hypoglycemia|Opioid-Related Severe Adverse Drug Event|Hospital Acquired Pressure Ulcer|Adverse Drug Event|Severe Hospital Acquired Delerium|Rapid Response Related to Arrhythmia Brigham and Women''s Hospital|Northeastern University April 2015 Not Applicable
NCT00568789 Completed Drug: Ramelteon zolpidem and placebo Insomnia Takeda June 2006 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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