Trial reportScientific reports2016
Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man.
Trial report in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
38 citing papers in PubMed, 80 citations in OpenAlex.
- Effects of the selective orexin-2 receptor antagonist JNJ-48816274 on sleep initiated in the circadian wake maintenance zone: a randomised trial.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Trial
- Sleep regulates drug seeking and relapse - a perspective.Molecular psychiatry · 2026Review
- Social defeat stress responses in the stress alternative model are dependent on sex and anterior basolateral amygdala orexin 2 receptors.Biology of sex differences · 2026Article
- Estimation of the Orexin Receptor Occupancy From Human Plasma Pharmacokinetics of Vornorexant, a Novel Dual Orexin 1/2 Receptor Antagonist for the Treatment of Insomnia.Pharmacology research & perspectives · 2026Article
- Beyond traditional sleeping pills: safety, efficacy and multidisease potential of three approved orexin receptor antagonists.Frontiers in psychiatry · 2026Review
- Neurophysiological differences between dexmedetomidine sedation and natural sleep across the rodent lifespan: implications for aging and perioperative brain health.Anesthesiology and perioperative science · 2026Article
- Found in translation: orexin receptor antagonism for the treatment of opioid use disorder.Translational psychiatry · 2025Review
- Review
- Hypocretin-1 receptor antagonism improves inhibitory control during the Go/No-Go task in highly motivated, impulsive male mice.Psychopharmacology · 2024Article
- Effects of methamphetamine on actigraphy-based sleep parameters in female rhesus monkeys: Orexin receptor mechanisms.Drug and alcohol dependence · 2024Article
- Readjustment of circadian clocks by exercise intervention is a potential therapeutic target for sleep disorders: a narrative review.Physical activity and nutrition · 2024Article
- The Orexin/Hypocretin System, the Peptidergic Regulator of Vigilance, Orchestrates Adaptation to Stress.Biomedicines · 2024Review
- Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats.RSC medicinal chemistry · 2024Article
- Structure and function of neocortical layer 6b.Frontiers in cellular neuroscience · 2023Review
- Differential sleep/wake response and sex differences following acute suvorexant, MK-1064 and zolpidem administration in the rTg4510 mouse model of tauopathy.British journal of pharmacology · 2022Article
- Translational approaches to influence sleep and arousal.Brain research bulletin · 2022Review
- Roles of Neuropeptides in Sleep-Wake Regulation.International journal of molecular sciences · 2022Review
- Interactions between Sleep and Emotions in Humans and Animal Models.Medicina (Kaunas, Lithuania) · 2022Review
- Discovery of Arylsulfonamides as Dual Orexin Receptor Agonists.Journal of medicinal chemistry · 2021Article
- Circadian rhythm as a therapeutic target.Nature reviews. Drug discovery · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
19 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Orexin neuropeptides regulate sleep/wake through orexin receptors (OX1R, OX2R); OX2R is the predominant mediator of arousal promotion. The potential for single OX2R antagonism to effectively promote sleep has yet to be demonstrated in humans. MK-1064 is an OX2R-single antagonist. Preclinically, MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. Similar to dual antagonists, MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy. Two Phase I studies in healthy human subjects evaluated safety, tolerability, pharmacokinetics and sleep-promoting effects of MK-1064, and demonstrated dose-dependent increases in subjective somnolence (via Karolinska Sleepiness Scale and Visual Analogue Scale measures) and sleep (via polysomnography), including increased REM and NREM sleep. Thus, selective OX2R antagonism is sufficient to promote REM and NREM sleep across species, similarly to that seen with dual orexin receptor antagonism.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.