TAK 375

Biological Activity

TAK 375 is a very high affinity and selective melatonin agonist (K_i values are 14 and 112 pM for human MT₁ and MT₂, respectively). Selective for human MT₁ and MT₂ over hamster MT₃ and a range of other targets including benzodiazepine, opiate and dopamine receptors, ion channels and transporters. Accelerates return to normal circadian rhythm in rats after phase shift, without affecting learning and memory. Also reduces infarct size in rat heart in vitro post ischemia-reperfusion.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Ramelteon (TAK-375) accelerates reentrainment of circadian rhythm after a phase advance of the light-dark cycle in rats
   Hirai et al.
   J.Biol.Rhythms., 2005;20:27
2. Melatonin receptor agonist rame. reduces ischemia-reperfusion injury through activation of mitochondrial potassium channels.
   Stroethoff et al.
   J.Cardiovasc.Pharmacol., 2018;72:106
3. Neurochemical properties of rame. (TAK-375), a selective MT1/MT2 receptor agonist.
   Kato et al.
   Neuropharmacology., 2005;48:301

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