The Involvement of 5-HT2A Receptor in the Regulation of Sleep and Wakefulness, and the Potential Therapeutic Use of Selective 5-HT2A Receptor Antagonists and Inverse Agonists for the Treatment of an Insomnia Disorder
| Autor: | Pablo Torterolo, D. Warren Spence, Jaime M. Monti, Seithikurippu R. Pandi Perumal |
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| Rok vydání: | 2018 |
| Předmět: |
Sleep induction
business.industry medicine.drug_class 05 social sciences Suvorexant Ramelteon Pharmacology Receptor antagonist 050105 experimental psychology Melatonin 03 medical and health sciences 0302 clinical medicine mental disorders medicine Inverse agonist 0501 psychology and cognitive sciences business Melatonin receptor agonist 030217 neurology & neurosurgery medicine.drug Slow-wave sleep |
| Zdroj: | 5-HT2A Receptors in the Central Nervous System ISBN: 9783319704722 |
| DOI: | 10.1007/978-3-319-70474-6_13 |
| Popis: | Several agents have been shown to improve sleep induction and/or maintenance in patients with primary or comorbid insomnia. These include benzodiazepine and non-benzodiazepine receptor allosteric modulators, melatonin and the melatonin receptor agonist ramelteon, low dose doxepin, and suvorexant. However, benzodiazepines induce a further reduction of N3 sleep [slow wave sleep (SWS) or delta sleep] and rapid-eye-movement sleep (REMS), whereas values corresponding to these variables remain decreased during non-benzodiazepine, melatonin, ramelteon or low-dose doxepin administration. By contrast, suvorexant increases REMS. There is evidence indicating that non-selective (ritanserin, ketanserin, sertindole, ICI-170809, ICI-169369, RP-62203, SR-46349B) and selective (volinanserin, pruvanserin, eplivanserin) 5-HT2A receptor antagonists, as well as 5-HT2A receptor inverse agonists (nelotanserin, pimavanserin) increase SWS in laboratory animals and N3 sleep in subjects with normal sleep and/or patients with an insomnia disorder. Thus, the association of a selective 5-HT2A receptor antagonist or a 5-HT2A receptor inverse agonist with a hypnotic drug could be a valid alternative to normalize N3 sleep in patients with an insomnia complaint. |
| Databáze: | OpenAIRE |
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