New substituted naphthalene derivatives are melatonin 1 receptor binders useful e.g. to treat sleep disorders, stress, anxiety, schizophrenia, panic attacks, appetite disorders, obesity, insomnia, epilepsy, diabetes and Parkinson's disease

摘要

N-[2-hydroxy-2-(7-methoxy-1-naphthyl)ethyl]propionamide (I) or its enantiomer and base addition salt is new. An independent claim is included for the preparation of (I). ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; CNS-Gen; Muscular-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Cytostatic; Dermatological; Vasotropic; Immunomodulator; Contraceptive; Analgesic. MECHANISM OF ACTION : Melatonin 1 (MT 1) receptor binder; MT 2 receptor binder; 5-HT2c receptor binder. The ability of (I) to bind MT 2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin radioligand. The result showed that inhibitory constant of N-[2-hydroxy-2-(7-methoxy-1-naphthyl)ethyl]propionamide was 0.3 nM.