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

Sharpley, A L; Elliott, J.M.; Attenburrow, Mary-Jane; Cowen, Philip J.

doi:10.1016/0028-3908(94)90077-9

Cited by 105 publications

(64 citation statements)

References 12 publications

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“…Results on sleep initiation and maintenance measures, as well as on SWS, are in concordance with previous reports where olanzapine was found to improve sleep continuity and produce dose-related SWS increases in schizophrenic (Salin-Pascual et al 2004) and healthy volunteers (Sharpley et al 2000;Lindberg et al 2002). Olanzapine is a potent 5-HT 2A/2C antagonist, and studies in humans and animals have shown that 5-HT 2A/2C receptors, primarily 5-HT 2C , are involved in the regulation of SWS (Sharpley et al 1994). Accordingly, it has been calculated that the 50% increase in SWS observed after olanzapine (5 mg) corresponds to a central occupancy of 5-HT 2C receptors of at least 70%.…”

Section: Discussionsupporting

confidence: 90%

Effects of olanzapine, risperidone and haloperidol on sleep after a single oral morning dose in healthy volunteers

et al. 2007

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Objectives To compare the effects of typical and atypical antipsychotic drugs on sleep activity and subjective sleep quality. Design Randomised, double-blind, placebo-controlled, four-period cross-over, clinical trial was used to evaluate the effects of active treatments on objective and subjective sleep variables. Setting Sleep laboratory evaluation. Participants Twenty healthy young volunteers, both sexes. Interventions Single oral morning administrations of olanzapine 5 mg, risperidone 1 mg, haloperidol 3 mg and placebo. Measurements and results Five polysomnographic nights were evaluated: one control night and one after each intervention. Significant increase in total sleep time, sleep efficiency, slow wave sleep (SWS) and rapid eye movement (REM) sleep with decreases in wake time were observed after olanzapine. Decreases in wake time, REM sleep and stage shifts together with increases in stage 2 were obtained after risperidone. Haloperidol showed only a tendency to increase sleep efficiency and stage 2 and to decrease wake time. Olanzapine showed decreases in power density in frequencies higher than 10 Hz during all sleep stages and in frequencies lower than 5 Hz range in SWS; decreases in the dynamics of spindle frequency activity (SFA) in the second and fourth non-rapid eye movement (NREM) episodes were also obtained. Risperidone presented increases in the 3.6-10.8 Hz frequency range in NREM sleep stages and in stage 2. Haloperidol also showed increases in NREM sleep stages and in stage 2, but these were in frequencies higher than 10 Hz, with increases in the dynamics of SFA in the first NREM episode. Only a significant improvement in subjective sleep quality was observed after olanzapine. Conclusions Antipsychotics showed different sleep changes as their neurochemical profiles were distinct. These changes were observed even when the drug was administered 15 h before going to bed.

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Section: Discussionsupporting

confidence: 90%

Effects of olanzapine, risperidone and haloperidol on sleep after a single oral morning dose in healthy volunteers

et al. 2007

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“…5-HT 1A agonists have been shown to suppress REM sleep (Driver et al 1995;Gillin et al 1994). Regarding SWS, drugs antagonising 5-HT 2A or 5-HT 2C demonstrate an enhancing effect on SWS (Landolt et al 1999;Sharpley et al 1994), whereas 5-HT 2C agonists appear to lower SWS (Katsuda et al 1993).…”

Section: Discussionmentioning

confidence: 99%

Daytime Ayahuasca administration modulates REM and slow-wave sleep in healthy volunteers

et al. 2007

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Objectives Ayahuasca is a traditional South American psychoactive beverage and the central sacrament of Brazilianbased religious groups, with followers in Europe and the United States. The tea contains the psychedelic indole N, N-dimethyltryptamine (DMT) and β-carboline alkaloids with monoamine oxidase-inhibiting properties that render DMT orally active. DMT interacts with serotonergic neurotransmission acting as a partial agonist at 5-HT 1A and 5-HT 2A/2C receptor sites. Given the role played by serotonin in the regulation of the sleep/wake cycle, we investigated the effects of daytime ayahuasca consumption in sleep parameters. Measurements and results Subjective sleep quality, polysomnography (PSG), and spectral analysis were assessed in a group of 22 healthy male volunteers after the administration of a placebo, an ayahuasca dose equivalent to 1 mg DMT kg −1 body weight, and 20 mg d-amphetamine, a proaminergic drug, as a positive control. Results show that ayahuasca did not induce any subjectively perceived deterioration of sleep quality or PSG-measured disruptions of sleep initiation or maintenance, in contrast with damphetamine, which delayed sleep initiation, disrupted sleep maintenance, induced a predominance of 'light' vs 'deep' sleep and significantly impaired subjective sleep quality. PSG analysis also showed that similarly to damphetamine, ayahuasca inhibits rapid eye movement (REM) sleep, decreasing its duration, both in absolute values and as a percentage of total sleep time, and shows a trend increase in its onset latency. Spectral analysis showed that d-amphetamine and ayahuasca increased power in the high frequency range, mainly during stage 2. Remarkably, whereas slow-wave sleep (SWS) power in the first night cycle, an indicator of sleep pressure, was decreased by d-amphetamine, ayahuasca enhanced power in this frequency band.Conclusions Results show that daytime serotonergic psychedelic drug administration leads to measurable changes in PSG and sleep power spectrum and suggest an interaction between these drugs and brain circuits modulating REM and SWS.

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“…The 75 mg dose of MDMA was selected because it falls within the normal range of and has been consistently shown to impair memory performance and produce robust subjective mood changes in a number of previous studies from our lab Ramaekers, 2005, 2007;Kuypers et al, 2006;Ramaekers et al, 2009). Doses of pindolol 20 mg and ketanserin 50 mg represent regular therapeutic doses that block B40% of 5HT 1A receptors and 91% of 5HT 2 receptors, respectively (Brogden and Sorkin, 1990;Rabiner et al, 2000;Sharpley et al, 1994).…”

Section: Treatments and Proceduresmentioning

confidence: 99%

Blockade of 5-HT2 Receptor Selectively Prevents MDMA-Induced Verbal Memory Impairment

Wel

Kuypers

Theunissen

et al. 2011

Neuropsychopharmacol

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3,4-Methylenedioxymethamphetamine (MDMA) or 'ecstasy' has been associated with memory deficits during abstinence and intoxication. The human neuropharmacology of MDMA-induced memory impairment is unknown. This study investigated the role of 5-HT 2A and 5-HT 1A receptors in MDMA-induced memory impairment. Ketanserin is a 5-HT 2A receptor blocker and pindolol a 5-HT 1A receptor blocker. It was hypothesized that pretreatment with ketanserin and pindolol would protect against MDMA-induced memory impairment. Subjects (N ¼ 17) participated in a double-blind, placebo-controlled, within-subject design involving six experimental conditions consisting of pretreatment (T1) and treatment (T2). T1 preceded T2 by 30 min. T1-T2 combinations were: placebo-placebo, pindolol 20 mg-placebo, ketanserin 50 mg-placebo, placebo-MDMA 75 mg, pindolol 20 mg-MDMA 75 mg, and ketanserin 50 mg-MDMA 75 mg. Memory function was assessed at Tmax of MDMA by means of a word-learning task (WLT), a spatial memory task and a prospective memory task. MDMA significantly impaired performance in all memory tasks. Pretreatment with a 5-HT 2A receptor blocker selectively interacted with subsequent MDMA treatment and prevented MDMA-induced impairment in the WLT, but not in the spatial and prospective memory task. Pretreatment with a 5-HT 1A blocker did not affect MDMA-induced memory impairment in any of the tasks. Together, the results demonstrate that MDMA-induced impairment of verbal memory as measured in the WLT is mediated by 5-HT 2A receptor stimulation.

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

Cited by 105 publications

References 12 publications

Effects of olanzapine, risperidone and haloperidol on sleep after a single oral morning dose in healthy volunteers

Effects of olanzapine, risperidone and haloperidol on sleep after a single oral morning dose in healthy volunteers

Daytime Ayahuasca administration modulates REM and slow-wave sleep in healthy volunteers

Blockade of 5-HT2 Receptor Selectively Prevents MDMA-Induced Verbal Memory Impairment

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