The Efficacy and Safety of the Melatonin Agonist beta-Methyl-6-Chloromelatonin in Primary Insomnia

International Union of Basic and Clinical Pharmacology. LXXV. Nomenclature, Classification, and Pharmacology of G Protein-Coupled Melatonin Receptors

“…7C). PD 6735 did not negatively affect other sleep parameters or produce morning-after psychomotor impairment (Mulchahey et al, 2004;Zemlan et al, 2005). PD 6735 did not cause hypothermia, hypertension, or bradycardia.…”

Promotion of Non-Rapid Eye Movement Sleep and Activation of Reticular Thalamic Neurons by a Novel MT2Melatonin Receptor Ligand

“…Three novel nonselective MT 1 /MT 2 agonists, TIK-301 (Zemlan et al, 2005), ramelteon (Mini et al, 2007), and tasimelteon (Rajaratnam et al, 2009), have been tested in humans for the treatment of insomnia; all three significantly reduced the latency to sleep, but were less potent in potentiating the long-term enhancement of total sleep time and without selectivity toward NREMS or REMS. The nonselective antidepressant MT 1 /MT 2 agonist agomelatine improves sleep after 6 weeks of treatment (Quera Salva et al, 2007), but its mechanisms of action remain to be elucidated, as it also binds to serotonergic 5-HT 2B and 5-HT 2C receptors, already known to be involved in sleep (Den Boer et al, 2006).…”

Influence of the novel antidepressant and melatonin agonist/serotonin2C receptor antagonist, agomelatine, on the rat sleep–wake cycle architecture

“…Moreover, numerous studies have reported a lack of correlation between endogenous levels of melatonin at night and sleep quality (Hughes et al 1998;Mahlberg and Kunz 2007). Accordingly, the decreased sleep latency observed after treatment with melatonin or melatonin agonists in insomniacs and patients with "delayed sleep phase syndrome" is probably related to phase-shifting effects rather than an impact on sleep per se (Mundey et al 2005;Zemlan et al 2005;Roth et al 2005).…”