Slow wave sleep in humans: role of 5-HT2A and 5-HT2C receptors

Neuropharmacology. 1994 Mar-Apr;33(3-4):467-71. doi: 10.1016/0028-3908(94)90077-9.


We studied the effects of the 5-HT2 receptor antagonists, ritanserin and ketanserin, on the sleep of healthy volunteers in order to clarify the role of 5-HT2A and 5-HT2C receptors in the regulation of slow wave sleep (SWS) in humans. Ritanserin, 5 mg, produced a substantially larger increase in SWS (51.4%) than either ketanserin, 20 mg (17.2%) or ketanserin, 40 mg (24.4%). Ritanserin has a significantly higher affinity than ketanserin for 5-HT2C receptor binding sites in the human brain and, based on estimates of per cent occupancy by the two compounds at brain 5-HT2A and 5-HT2C receptors, we conclude that SWS in humans is primarily regulated by 5-HT2C receptors.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Brain Chemistry / physiology
  • Female
  • Humans
  • Ketanserin / pharmacology
  • Male
  • Polysomnography
  • Radioligand Assay
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / physiology*
  • Ritanserin / pharmacology
  • Serotonin Antagonists / pharmacology
  • Serotonin Receptor Agonists / pharmacology
  • Sleep / drug effects*
  • Sleep, REM / drug effects


  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • Ritanserin
  • Ketanserin