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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.

Type

Journal article

Journal

Neuropharmacology

Publication Date

03/1994

Volume

33

Pages

467 - 471

Keywords

Adult, Brain Chemistry, Female, Humans, Ketanserin, Male, Polysomnography, Radioligand Assay, Receptors, Serotonin, Ritanserin, Serotonin Antagonists, Serotonin Receptor Agonists, Sleep, Sleep, REM