| Name | Ramelteon |
| Description | Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist. |
| Kinase Assay | cDNA encoding the human MT1 gene is introduced into CHO cells. Cells are harvested at confluence in Ca2+ and Mg2+ free Hanks' balanced salt solution containing 5 mM EDTA and collected by centrifugation. Cells are homogenized in ice-cold 50 mM Tris–HCl buffer, washed twice, pelleted, and stored at -30°C until the binding assays are conducted. Test compound and 40 pM 2-[ 125I]melatonin are mixed with the thawed homogenate in a total volume of 1 mL and incubated at 25°C for 150 min. The reaction is terminated by addition of 3 mL of icecold buffer followed by vacuum filtration on a Whatman GF/B. The filter is washed twice and radioactivity is counted by a g-counter[1]. |
| In vitro | Ramelteon inhibited melanocyte pigment granule aggregation in the African clawed toad (Xenopus laevis) with a pEC50 of 11.48.1 nM Ramelteon increased ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells, but also in cerebellar granule cells containing only one melatonin receptor.Ramelteon inhibits forskolin-stimulated cAMP production with an IC50 of 21.2 pM in CHO cells. 4P-PDOT blocked the stimulatory effect of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, whereas luzindole attenuated the effect of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon showed high affinity for recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. |
| In vivo | Ramelteon inhibited melanocyte pigment granule aggregation in the African clawed toad (Xenopus laevis) with a pEC50 of 11.48.1 nM Ramelteon increased ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells, but also in cerebellar granule cells containing only one melatonin receptor.Ramelteon inhibits forskolin-stimulated cAMP production with an IC50 of 21.2 pM in CHO cells. 4P-PDOT blocked the stimulatory effect of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, whereas luzindole attenuated the effect of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon showed high affinity for recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. |
| Storage | Store at low temperature | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7.71 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 49 mg/mL (188.94 mM), Sonication is recommended.
DMSO : 166.7 mg/mL (642.79 mM), Sonication is recommended.
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| Keywords | withdrawal symptom | TAK375 | TAK 375 | rebound insomnia | Ramelteon | oral | next-morning residual effect | MTReceptor | MT2 receptor | MT2 | MT1 receptor | MT1 | MT receptor (chicken) | MT Receptor | MelatoninReceptor | Melatonin Receptor | insomnia | Inhibitor | inhibit | discontinuation |
| Inhibitors Related | Agomelatine | ACH-000143 | glycine | Methyl Linolenate | 6-Chloromelatonin | 4-P-PDOT | Tasimelteon | Agomelatine (L(+)-Tartaric acid) | UCM 608 | Melatonin | Piromelatine | Luzindole |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Drug Library |
United States
