Reference

Novel naphthalenic ligands with high affinity for the melatonin receptor

Novel naphthalenic ligands with high affinity for the melatonin receptor. Yous, S.Several substances are used for example 138112-76-2 and 58881-45-1 which are their cas registry numbers.; Andrieux, J.; Howell, H. E.; Morgan, P. J.; Renard, P.; Pfeiffer, B.; Lesieur, D.; Guardiola-Lemaitre, B. (Fac. Pharm., Lille, Fr.). J. Med. Chem., 35(8), 1484-6 (English) 1992. CODEN: JMCMAR. ISSN: 0022-2623. DOCUMENT TYPE: Journal CA Section: 25 (Benzene, Its Derivatives, and Condensed Benzenoid Compounds) Section cross-reference(s): 1 Fifteen naphthalenic bioisosteres I [R = Me, Et, Pr, Bu, pentyl, hexyl, Me2CH, crotyl, cyclopropyl, cyclobutyl, cyclohexyl, PhCH2, Ph, 3,5-(Cl)2C6H3, 2-indolyl] of melatonin with variations on the N-acylamino group were synthesized from (7-methoxy-1-naphthyl)acetic acid and evaluated for their binding affinity for the melatonin receptor. Some of these ligands, e.g., I (R = cyclopropyl), show greater affinity (10 to 100 fold) than melatonin itself. The results of this study provide new and useful information about the structure-binding relationships and mode of interaction at the melatonin receptor. .

Could agomelatine be the ideal antidepressant?

All Rights Reserved. Could agomelatine be the ideal antidepressant?. Pandi-Perumal, S. R.; Srinivasan, V.; Cardinali, D. P.; Monti, J. M.Some commonly used reagents like 138112-76-2 is used in this experiment. ( Comprehensive Center for Sleep Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, Mount Sinai School of Medicine, New York, NY 10029, USA). Expert Review of Neurotherapeutics, 6(11), 1595-1608 (English) 2006 Future Drugs Ltd. CODEN: ERNXAR. ISSN: 1473-7175. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. Depressive disorders are a common cause of chronic and recurrent psychiatric dysfunction, constituting the fourth leading cause of global diseases. Depression is assocd. with a high rate of morbidity and mortality, and is a leading cause of global disability. Despite the effectiveness of most currently available antidepressants, many of them have a no. of undesirable side effects. Agomelatine is the first melatonin (MT)1/MT2 agonist having 5-hydroxytryptamine (5-HT)2C and 5-HT2B antagonist properties and antidepressant activity. Agomelatine is effective in several animal models of depression and anxiety. In addn., three large, multicenter, multinational, placebo-controlled studies and several double-blind, placebo-controlled trials of agomelatine have demonstrated that it is a clin. effective and well-tolerated antidepressant in acute trials. Since currently available antidepressants are not always adequate to cause complete remission of symptoms in severely depressed patients, the superior rate of response achieved with agomelatine in this group of patients underlines its future for clin. use in depressive disorders. In summary, the clin. advantage of agomelatine is attributed to its novel mechanism of action, which helps not only to exert antidepressant action, but also to regulate the sleep-wake rhythm. .