Slow wave sleep in humans: role of 5-HT2A and 5-HT2C receptors.
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.
Sharpley
A L
AL
Psychopharmacology Research Unit, Littlemore Hospital, Oxford, U.K.
Elliott
J M
JM
Attenburrow
M J
MJ
Cowen
P J
PJ
D000328:Adult; D001923:Brain Chemistry / Q000502:physiology; D005260:Female; D006801:Humans; D007650:Ketanserin / Q000494:pharmacology; D008297:Male; D017286:Polysomnography; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000187:drug effects / Q000502:physiology*; D016713:Ritanserin / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000494:pharmacology; D012890:Sleep / Q000187:drug effects*; D012895:Sleep, REM / Q000187:drug effects
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D016713:Ritanserin; D007650:Ketanserin