Abstract
The effects of the selective 5-HT2 receptor antagonists, ritanserin (1, 5 and 10 mg) and ICI 169,369 (50 and 100 mg), were studied on the sleep EEG of healthy volunteers using home-based Medilog 9000 cassette monitoring. Ritanserin (5 and 10 mg) produced a significant increase in slow wave sleep (SWS) while ICI 169,369 also increased SWS but only at a dose of 100 mg. These findings are consistent with the proposal that selective 5-HT2 receptor blockade increases SWS in humans; however, the data cannot exclude involvement of the closely related 5-HT1c receptor in this effect.
References
Adam K, Oswald I (1989) Effects of repeated ritanserin on middle-aged poor sleepers. Psychopharmacology 99:219–221
Blackburn TP, Cox B, Pearce RJ, Thornber CW (1987a) In vitro pharmacology of ICI 169,369 — a new 5-HT2 antagonist. Br J Pharmacol 90:227P
Blackburn TP, Cox B, Pearce RJ, Thornber CW (1987b) In vivo pharmacology of ICI 169,369 — a new 5-HT2 antagonist. Br J Pharmacol 90:256P
Blackburn TP, Cox B, Thornber CW, Pearce RJ (1990) Pharmacological studies in vivo with ICI 169,369, a chemically novel 5-HT2/5-HT1c receptor antagonist. Eur J Pharmacol (in press)
Dugovic C, Waquier A (1987) 5-HT2 receptors could be primarily involved in the regulation of slow wave sleep in the rat. Eur J Pharmacol 137:145–146
Friston KJ, Sharpley AL, Solomon RA, Cowen PJ (1989) Lithium increases slow wave sleep: possible mediation by brain 5-HT2 receptors? Psychopharmacology 98:139–140
Genco S, Puca FM, Specchio LM, Interno S, Castriott R, Leomanni R, Dammacco F (1977) Metergolina e sonno notturnonell'uomo normale. Boll Soc Ital Biol Sper 53:1403–1406
Hartig PR (1989) Molecular biology of 5-HT receptors. TIPS 10:64–69
Hoyer D (1988) Molecular pharmacology and biology of 5-HT1c receptors. TIPS 9:89–94
Idzikowski C, Mills FJ (1987) A dose-response study of the effects of ritanserin on slow wave sleep. Sleep Res 16:93
Idzikowski C, Mills FJ, Glennard R (1986) 5-Hydroxytryptamine-2 antagonist increases human slow wave sleep. Brain Res 378:164–168
Leysen JE, Awouters F, Kennis L, Laduron PM, Vandenberk J, Janssen PAJ (1981) Receptor binding profile of R 41468, a novel antagonist at 5-HT2 receptors. Life Sci 28:1115–1122
Mendelson WB, Reichman J, Othmer E (1975) Serotonin inhibition and sleep. Biol Psychiatry 10:459–464
Solomon RA, Sharpley AL, Cowen PJ (1989) Increased slow wave sleep with 5-HT2 receptor antagonists: detection by ambulatory EEG recording and automatic sleep stage analysis. J Psychopharmacol 3:125–129
Specchio LM, Puca FM, Genco S, Candeliere G, Galeone D, Dammacco F (1976) Effectti della ciproeptadina sul sonno delluomo normale. Boll Soc Ital Biol Sper 52:1789–1793
Tortella FC, Eschevaria E, Pastel RH, Cox B, Blackburn TP (1989) Antidepressant effects of selective 5-HT2 antagonists on rapid eye movement sleep in rats. Brain Res 485:294–300
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Sharpley, A.L., Solomon, R.A., Fernando, A.I. et al. Dose-related effects of selective 5-HT2 receptor antagonists on slow wave sleep in humans. Psychopharmacology 101, 568–569 (1990). https://doi.org/10.1007/BF02244239
Received:
Revised:
Issue Date:
DOI: https://doi.org/10.1007/BF02244239