+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat



Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat



European Journal of Pharmacology 553(1-3): 163-170



The effects of the serotonin 5-HT(2A/2C) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and of the selective 5-HT(2A) or 5-HT(2C) receptor antagonists 7-{4-[2-(4-fluoro-phenyl)-ethyl]-piperazine-1-carbonyl}-1H-indole-3-carbonitrile HCl (EMD 281014) and 5-methyl-1-[[-2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylindoline HCl (SB-243213), respectively, on spontaneous sleep were studied in adult rats implanted for chronic sleep recordings. Subcutaneous administration of DOI (0.35-0.7 mmol/kg) significantly increased waking and light sleep and reduced slow wave sleep, rapid-eye-movement (REM) sleep, and the number of REM periods. With subcutaneous EMD 281014 (1.2-4.8 mmol/kg) or SB-243213 (1.2-4.8 mmol/kg) a significant reduction in time spent in REM sleep was also seen. Pretreatment with EMD 281014 prevented the DOI-induced increase of waking and light sleep and the reduction of slow wave sleep. However, REM sleep remained suppressed. SB-243213 failed to reverse the changes of sleep and waking induced by DOI. Thus, on the basis of these results it appears that serotonin 5-HT(2A) receptor mechanisms might be responsible for the DOI-induced effects on waking and slow wave sleep.

Please choose payment method:






(PDF emailed within 0-6 h: $19.90)

Accession: 012855370

Download citation: RISBibTeXText

PMID: 17059817

DOI: 10.1016/j.ejphar.2006.09.027


Related references

EMD 281014, a new selective serotonin 5-HT2A receptor antagonist. European Journal of Pharmacology 473(2-3): 229-230, 25 July, 2003

(1R, 3S)-(-)-trans-PAT: a novel full-efficacy serotonin 5-HT2C receptor agonist with 5-HT2A and 5-HT2B receptor inverse agonist/antagonist activity. European Journal of Pharmacology 615(1-3): 1-9, 2009

Functional characteristics of serotonin 5-HT2A and 5-HT2C receptors in the brain and the expression of the 5-HT2A and 5-HT2C receptor genes in aggressive and non-aggressive rats. Neuroscience and Behavioral Physiology 40(4): 357-361, 2010

Antagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo. Journal of Pharmacology and Experimental Therapeutics 339(1): 99, 2011

Influence of serotonin 5-HT2A and 5-HT2C receptor agonists and antagonists on the locomotor and discriminative stimulus effects of cocaine or direct dopamine D1-like and D2-like receptor agonists. European Neuropsychopharmacology 13(Suppl. 4): S422-S423, 2003

Selective serotonin 5-HT2A receptor antagonist EMD 281014 improves delayed matching performance in young and aged rhesus monkeys. Psychopharmacology 179(4): 725-732, 2005

Dissociable effects of selective 5-HT2A and 5-HT2C receptor antagonists on serial spatial reversal learning in rats. Neuropsychopharmacology 33(8): 2007-2019, 2007

Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor. Journal of Pharmacological Sciences 102(2): 189-195, 2006

Differentiation of 5-HT2A and 5-HT2C receptor mediated behaviors with selective antagonists?. Society for Neuroscience Abstracts 24(1-2): 1370, 1998

Apd125, a Selective Serotonin 5-Ht2A Receptor Inverse Agonist, Significantly Improves Sleep Maintenance in Primary Insomnia. Sleep 31(12): 1663-1671, 2008

Effects of the 5-HT2C receptor agonist Ro60-0175 and the 5-HT2A receptor antagonist M100907 on nicotine self-administration and reinstatement. Neuropharmacology 62(7): 2288-2298, 2012

Functional correlates of the brain 5-HT2A and 5-HT2C serotonin receptors and expression of 5-HT2A AND 5-HT2C genes in aggressive and nonaggressive Norway rats. Rossiiskii Fiziologicheskii Zhurnal Imeni I.M. Sechenova 95(2): 99, 2009

Serotonin 5-HT2A but not 5-HT2C receptor antagonism reduces hyperlocomotor activity induced in dopamine-depleted rats by striatal administration of the D1 agonist SKF 82958. Neuropharmacology 49(3): 350-358, 2005

5-HT2A and 5-HT2C receptor antagonists have opposing effects on a measure of impulsivity: interactions with global 5-HT depletion. Psychopharmacology 176(3-4): 376-385, 2004

Position 5.46 of the serotonin 5-HT2A receptor contributes to a species-dependent variation for the 5-HT2C agonist (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one: impact on selectivity and toxicological evaluation. Molecular Pharmacology 76(6): 1211-1219, 2009