ArticleNature and science of sleep2010
Role of 5-HT2A receptor antagonists in the treatment of insomnia.
Article in Nature and science of sleep, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers, 1 of them a synthesis that pooled it.
What it found
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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
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 54 citations in OpenAlex.
- A Meta-Analysis of the Effects of Acute Sleep Deprivation on the Cortical Transcriptome in Rodent Models.Journal of sleep research · 2026Pooled it
- Pimavanserin tartrate, a 5-HT(2A) receptor inverse agonist, increases slow wave sleep as measured by polysomnography in healthy adult volunteers.Sleep medicine · 2011Trial
- Adjunctive Pharmacotherapy for Major Depressive Disorder with Anxiety Symptoms: from Monoamines to Recent Clinical Evidence.CNS drugs · 2026Review
- Article
- Effects of adjunctive brexpiprazole in patients with major depressive disorder and sleep disturbance: aFrontiers in psychiatry · 2025Article
- Pharmacologic profile of ITI-333: a novel molecule for treatment of substance use disorders.Psychopharmacology · 2024Article
- Exploring cariprazine as a treatment option for varied depression symptom clusters.Frontiers in psychiatry · 2024Review
- Neuropharmacological Activities ofPharmaceuticals (Basel, Switzerland) · 2022Article
- Psilocin acutely alters sleep-wake architecture and cortical brain activity in laboratory mice.Translational psychiatry · 2022Article
- 2-Phenyl-1ACS chemical neuroscience · 2021Article
- Pimavanserin, a 5HTJournal of neurochemistry · 2021Article
- Identification of a Potent and Selective 5-HTACS chemical neuroscience · 2020Article
- Structures of the 5-HTNature structural & molecular biology · 2019Article
- Two combined amino acids promote sleep activity in caffeine-induced sleepless model systems.Nutrition research and practice · 2018Article
- Serotonin and brain function: a tale of two receptors.Journal of psychopharmacology (Oxford, England) · 2017Review
- Mechanism Exploration of Arylpiperazine Derivatives Targeting the 5-HTMolecules (Basel, Switzerland) · 2017Article
- C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.Bioorganic & medicinal chemistry letters · 2015Article
- ITI-007 demonstrates brain occupancy at serotonin 5-HT₂A and dopamine D₂ receptors and serotonin transporters using positron emission tomography in healthy volunteers.Psychopharmacology · 2015Article
- Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor.Pharmacology research & perspectives · 2015Article
- Functional profile of a novel modulator of serotonin, dopamine, and glutamate neurotransmission.Psychopharmacology · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Insomnia encompasses a difficulty in falling asleep (sleep-onset insomnia) and/or a difficulty in staying asleep (SMI). Several selective serotonin-2A (5-HT2A) receptor antagonists have been in development as potential treatments for SMI. However, none have shown a sufficiently robust benefit-to-risk ratio, and none have reached market approval. We review the role of the 5-HT2A mechanism in sleep, the preclinical and clinical data supporting a role for 5-HT2A receptor antagonism in improving sleep maintenance, and the status of 5-HT2A receptor antagonists in clinical development. Overall, the polysomnography data strongly support an increase in slow-wave sleep and a decrease in waking after sleep onset following treatment with 5-HT2A receptor antagonists, although it has been more difficult to show subjective improvements in sleep with these agents. The incidence and prevalence of SMI, whether primary or secondary to psychiatric, neurologic, or other medical conditions, will increase as our population ages. There will be an increased need for safe and efficacious treatments of insomnia characterized by difficulty maintaining sleep, and there remains much promise for 5-HT2A receptor antagonism to play a role in these future treatments.
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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.