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

Sleep. 1992 Apr;15(2):119-24. doi: 10.1093/sleep/15.2.119.

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.

MeSH terms

  • Animals
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / 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*
  • Sleep Stages / physiology
  • Sleep, REM / drug effects
  • Sleep, REM / physiology
  • Wakefulness

Substances

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