Therapeutic potential of melatonin agonists

作者: Daniel P Cardinali , Seithikurippu R Pandi-Perumal , Venkataramanujan Srinivasan , D Warren Spence , Ilya Trakht

DOI: 10.1586/17446651.3.2.269

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摘要: Melatonin, a hormone secreted by the pineal gland, has been successfully employed to improve sleep in both normal patients and insomniacs, for treatment of circadian rhythm disorders. Melatonergic MT1 MT2 receptors exist high concentrations suprachiasmatic nucleus hypothalamus have shown be instrumental sleep-promoting rhythm-regulating effects melatonin. A lack consistency among reports on therapeutic efficacy melatonin attributed differences melatonin’s bioavailability short half-life hormone. In view need longer acting melatonergic agonists that efficiency without causing drug abuse or dependency, ramelteon (Rozerem™, Takeda) was developed. Ramelteon, which acts via MT1/MT2 agonism, found clinically effective improving total time insomniacs. Agomelatine (Valdoxan™, Servier) is another agonist...

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