Product Name: Ramelteon CAS 196597-26-9
Chemical & Physical Properties
Appearance : White to off-white Solid
Boiling Point:455.3℃ at 760 mmHg
Melting Point: 113-115℃
Ramelteon, marketed as Rozerem by Takeda Pharmaceuticals North America, is a sleep agent that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN), instead of binding to GABAA receptors, such as with drugs like zolpidem.
It however does not appear to speed the onset of sleep or the amount of sleep a person gets. It is approved by the U.S. Food and Drug Administration (FDA) for long-term use.
Ramelteon does not show any appreciable binding to GABAA receptors, which are associated with anxiolytic, myorelaxant, and amnesic effects.
Ramitelon, trade name: rozerem, chemical name (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, approved by FDA to be listed in the United States in September 2005, trade name: rozerem, can be used for the treatment of insomnia of difficult to sleep type, and has definite effect on chronic insomnia and short-term insomnia. This product can selectively activate melatonin type 1 receptor and type 2 receptor (MT1, MT2), increase slow wave sleep (SWS) and rapid eye movement sleep (rew), so as to reduce insomnia.
Rimetidine is the first non addictive insomnia treatment drug not listed as a special control. The mechanism of action is that rimetidine is a chemical Book agonist of melatonin receptor, which has a high affinity with the MT1 and MT2 receptors of melatonin. In addition, it does not bind to neurotransmitter receptors such as GABA receptor complex, and does not interfere with the activity of most enzymes within a certain range. Therefore, it can avoid the distraction related to GABA drugs (which may lead to traffic accidents, falls and fractures), drug addiction and dependence. The total amount of its main metabolite M-II is 20-100 times of that of the mother, but its activity is relatively low. Its affinity with MT1 and MT2 receptors is about 1 / 5 and 1 / 10 of that of the mother, respectively. Compared with the original drug, its pharmacological activity is reduced by 17-25 times. Other metabolites of this product have no activity.
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