Effects of the selective activation of 5-HT3 receptors on sleep: a polysomnographic study in healthy volunteers.
The respective role of various classes of central serotonin (5-HT) receptors in the regulation of sleep-wakefulness cycles has been the subject of many studies. Notably, it has been reported that 5-HT1A/B receptors are involved in the regulation of rapid eye movement sleep (REMS) and that 5-HT2A/C receptors participate in the control of slow wave sleep (SWS), but the role of 5-HT3 receptors is less well characterised. In this study we investigated the effects of SR 57227A, a potent and selective 5-HT3 agonist, on the sleep EEG of normal young male volunteers. SR 57227A (2.5, 5, 10, 20, 40 mg o.d. and 20 mg b.i.d.) or placebo were administered during 7 consecutive days in seven groups of ten subjects using a parallel group design. Sleep EEG recordings were performed on days 6 and 7 after an habituation session. SR 57227A produced a dose-dependent shift of REMS toward the end of the night without changing REMS and SWS duration nor altering sleep continuity. It suggests a role for the 5-HT3 receptor in the human sleep-wakefulness cycle and particularly in REMS regulation.
Staner
L
L
FORENAP-Institute for Research in Neurosciences, Neuropharmacology and Psychiatry, Centre Hospitalier, 27 rue du 4eme R.S.M., F-68250, Rouffach, France. luc.staner@forenap.asso.fr
Linker
T
T
Toussaint
M
M
Danjou
P
P
Roegel
J C
JC
Luthringer
R
R
Le Fur
G
G
Macher
J P
JP
D000293:Adolescent; D000328:Adult; D000704:Analysis of Variance; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004569:Electroencephalography / Q000187:drug effects; D006801:Humans; D008297:Male; D008875:Middle Aged; D010880:Piperidines / Q000494:pharmacology; D017286:Polysomnography / Q000187:drug effects / Q000379:methods; D011985:Receptors, Serotonin / Q000502:physiology*; D044406:Receptors, Serotonin, 5-HT3; D017366:Serotonin Receptor Agonists / Q000494:pharmacology; D012890:Sleep / Q000187:drug effects / Q000502:physiology*; D012895:Sleep, REM / Q000187:drug effects / Q000502:physiology
D010880:Piperidines; D011985:Receptors, Serotonin; D044406:Receptors, Serotonin, 5-HT3; D017366:Serotonin Receptor Agonists; C083009:4-amino-1-(6-chloro-2-pyridyl)piperidine hydrochloride