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

Abstract

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.

• Authors: J M Stutzmann, B Eon, M Lucas, J C Blanchard, P M Laduron
• Journal: Sleep (Sleep) Vol. 15 Issue 2 Pg. 119-24 (Apr 1992) ISSN: 0161-8105 [Print] United States
• PMID: 1579785 (Publication Type: Journal Article)

Chemical References

• Cyclic S-Oxides
• Naphthalenes
• Receptors, Serotonin
• Ritanserin
• fananserin

Topics

• Animals
• Cerebral Cortex (drug effects, physiology)
• Cyclic S-Oxides (pharmacology)
• Electroencephalography (drug effects)
• Female
• Humans
• Male
• Naphthalenes (pharmacology)
• Rats
• Receptors, Serotonin (drug effects)
• Ritanserin (pharmacology)
• Sleep (physiology)
• Sleep Stages (drug effects, physiology)
• Sleep, REM (drug effects, physiology)
• Wakefulness