product name Ramelteon
Description: Ramelteon (also known as 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 is the first in a new class of sleep agents that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN). Ramelteon does not show any appreciable binding to GABAA receptors, which are associated with anxiolytic, myorelaxant, and amnesic effects.
References: Neuropharmacology. 2005 Feb;48(2):301-10; J Pineal Res. 2008 Sep;45(2):125-32.
259.34
Formula
C16H21NO2
CAS No.
196597-26-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 52 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: 52 mg/mL (200.5 mM)
Solubility (In vivo)
0.5% methylcellulose: 30 mg/mL
Synonyms
TAK-375
other peoduct :
| In Vitro |
In vitro activity: Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. 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. |
| Animal model | Estrogen-deficient ovariectomized (OVX) rats |
| Formulation & Dosage | Dissolved in 0.5% methylcellulose solution; 1 mg/kg; oral gavage |
| References | Neuropharmacology. 2005 Feb;48(2):301-10; J Pineal Res. 2008 Sep;45(2):125-32. |
