RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats

• Published in: Sleep (New York, N.Y.) N.Y.), 1992-04, Vol.15 (2), p.119-124
• Main Authors: STUTZMANN, J.-M, EON, B, LUCAS, M, BLANCHARD, J.-C, LADURON, P. M
• Format: Article
• Language: English
• Subjects: Animals; Biological and medical sciences; Cerebral Cortex - drug effects; Cerebral Cortex - physiology; Cyclic S-Oxides - pharmacology; Electroencephalography - drug effects; Female; Fundamental and applied biological sciences. Psychology; Humans; Male; Naphthalenes - pharmacology; Rats; Receptors, Serotonin - drug effects; Ritanserin - pharmacology; Sleep - physiology; Sleep Stages - drug effects; Sleep Stages - physiology; Sleep, REM - drug effects; Sleep, REM - physiology; Sleep. Vigilance; Vertebrates: nervous system and sense organs; Wakefulness
• ISSN: 0161-8105; 1550-9109

RP 62203, a naphtosultam derivative, is an antagonist at the 5-hydroxytryptamine2 (HT2) receptor. The sleep pattern of rats treated orally with RP 62203 was studied at doses ranging from 0.5 to 4 mg/kg. Following RP 62203 administration, the duration of deep nonrapid eye movement (NREM) sleep was found to increase at the expense of wakefulness in a dose-dependent manner from 0.5 mg/kg. The 5-HT2 receptor agonist DOI and the 5-HT1a receptor agonist 8 OH-DPAT induced a dose-related increase in wakefulness; treatment with RP 62203 reversed the enhancement of wakefulness produced by DOI but not that produced by 8 OH-DPAT. These data provide further evidence for the involvement of 5-HT2 receptors in the regulation of NREM sleep in rats. RP 62203 could therefore be of clinical interest in the management of sleep disorders, particularly those developing within a psychiatric context.