Effects of activation and blockade of 5-HT2A/2C receptors in the dorsal raphe nucleus on sleep and waking in the rat

@article{Monti2006EffectsOA,
  title={Effects of activation and blockade of 5-HT2A/2C receptors in the dorsal raphe nucleus on sleep and waking in the rat},
  author={Jaime M. Monti and H{\'e}ctor Jantos},
  journal={Progress in Neuro-Psychopharmacology and Biological Psychiatry},
  year={2006},
  volume={30},
  pages={1189-1195}
}
  • J. Monti, H. Jantos
  • Published 30 September 2006
  • Psychology, Medicine
  • Progress in Neuro-Psychopharmacology and Biological Psychiatry
The effects of the 5-HT(2A/2C) receptor agonist DOI and of the selective 5-HT(2A) or 5-HT(2C) receptor antagonists EMD 281014 and SB-243213, respectively, on spontaneous sleep were studied in adult rats implanted for chronic sleep recordings. The serotonergic ligands were microinjected directly into the dorsal raphe nucleus (DRN). Infusion of DOI (1.4-5.6 mmol) into the DRN induced a significant reduction of REM sleep (REMS) and of the number of REM periods. Following the microinjection of EMD… 
Activation of the serotonin 5-HT3 receptor in the dorsal raphe nucleus suppresses REM sleep in the rat
  • J. Monti, H. Jantos
  • Chemistry, Medicine
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2008
TLDR
The effects of the selective 5-HT(3) receptor agonist and antagonist m-chlorophenylbiguanide and ondansetron were studied in adult male Wistar rats implanted for chronic sleep recordings and it is suggested that the suppression of REMS after the microinjection of m-CPBG into the DRN is related, at least in part, to the stimulation of glutamatergic interneurons that express 5- HT( 3) receptors.
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TLDR
The results suggest that 5-HT2C receptor blockade followed by blockade of CB1 receptors evoked additive effect on the regulation of sleep–wake pattern.
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TLDR
In the case of none subtype-selective compounds, the 5-HT2A receptor-mediated effects usually dominate the outcome on sleep-wake stages and thus, inhibition of non-REM sleep could be expected after administration of selective serotonin reuptake inhibitor antidepressants and atypical antipsychotic compounds, although high affinity to other compounds may mask the outcome in certain cases.
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Based on electrophysiological, neurochemical, and neuropharmacological approaches, it is currently accepted that serotonin (5-HT) functions to promote waking (W) and to inhibit (permissive role) REM
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TLDR
The results suggest that the on-off (activation/blockade), two-state ligand-receptor interaction model is not tenable for the 5-HT7 receptor.
Involvement of local orphanin FQ in the development of analgesic tolerance induced by morphine microinjections into the dorsal raphe nucleus of rats
TLDR
In MOR-tolerant rats, a single NST microinjection into the same DRN site was enough to restore the antinociceptive effect of MOR, and emphasizes the central importance of DRN-located OFQ in the MOR analgesic tolerance.
Serotonin control of sleep-wake behavior.
  • J. Monti
  • Psychology, Medicine
    Sleep medicine reviews
  • 2011
TLDR
5-HT(2A) and 5- HT(2C) receptor knock-out mice show a significant increase of W and a reduction of slow wave sleep (SWS) which has been ascribed to the increase of catecholaminergic neurotransmission involving mainly the noradrenergic and dopaminergic systems.
The role of dorsal raphe nucleus serotonergic and non-serotonergic neurons, and of their receptors, in regulating waking and rapid eye movement (REM) sleep.
  • J. Monti
  • Biology, Medicine
    Sleep medicine reviews
  • 2010
TLDR
Available evidence tends to indicate that non-5-HT cells contribute to the regulation of the activity of 5-HT neurons during the sleep-wake cycle through local circuits and/or their mediation of the effects of afferent inputs.
Serotonergic Systems in Sleep and Waking
TLDR
Emerging evidence now indicates that 5-HT DR neurons are a critical component of a complex neural circuitry in which the DR/MR plays a permissive role in rapid eye movement (REM) sleep, as their virtual silencing during REM disinhibits REM-active neurons to thus trigger the state of REM sleep.
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References

SHOWING 1-10 OF 35 REFERENCES
Functional role of 5-HT2 receptors in the regulation of sleep and wakefulness in the rat
TLDR
The hypothesis that the serotonergic system plays an active role in the regulation of the sleep-wakefulness cycle in the rat and that 5-HT2 receptors are involved in this action is supported.
Effects of the 5-HT1A receptor ligands flesinoxan and WAY 100635 given systemically or microinjected into the laterodorsal tegmental nucleus on REM sleep in the rat
TLDR
The effects of systemic flesinoxan on sleep variables may depend mainly on the activation of postsynaptic 5-HT1A receptors, whereas the effects corresponding to systemic WAY 100635 may be predominantly related to the blockade of presynaptic somatodendritic 5- HT1A autoreceptors.
Control of Serotonergic Function in Medial Prefrontal Cortex by Serotonin-2A Receptors through a Glutamate-Dependent Mechanism
TLDR
In vivo effects of 4-iodo-2,5-dimethoxyamphetamine reduce the activity of ascending 5-HT neurons through a DR-based action and enhances serotonergic and glutamatergic transmission in mPFC through 5- HT2A and AMPA receptors.
Effect of SB-243213, a selective 5-HT2C receptor antagonist, on the rat sleep profile A comparison to paroxetine
TLDR
The similar effect of SB-243213-A to paroxetine with regard to PS quantity provides further evidence that 5-HT(2C) receptor antagonists maybe beneficial in the treatment of depression/anxiety.
A serotonergic (5-HT2) receptor mechanism in the laterodorsal tegmental nucleus participates in regulating the pattern of rapid-eye-movement sleep occurrence in the rat
TLDR
Intervention of 5-HT(2) receptor sites with DOI and ketanserin decreased the occurrence of clusters of REM sleep episodes appearing at intervals less than or equal to 3 min without affecting single episodes separated by more than 3 min.
Inhibition of 5-hydroxytryptamine neuronal activity by the 5-HT agonist, DOI.
TLDR
Results suggest that the inhibition of 5-HT neuronal firing seen with administration of DOI is mediated via an action within the dorsal raphe and at least in close proximity to the5-HT neurone cell bodies.
Serotonin 5-HT2 receptors activate local GABA inhibitory inputs to serotonergic neurons of the dorsal raphe nucleus
TLDR
Results indicate that within the DRN–PAG area there may be a negative feedback loop in which 5-HT induces an increase in IPSC frequency in5-HT cells by exciting GABAergic interneurons in theDRN via 5-ht 2A and, to a lesser extent, 5- HT 2C receptors.
Biphasic effects of dopamine D-2 receptor agonists on sleep and wakefulness in the rat
TLDR
The increase in sleep after low doses of apomorphine, bromocriptine or pergolide could be related to activation of presynaptic D-2 receptors located on DA axons of mesolimbic and mesocortical systems and inhibition of norepinephrine and acetylcholine neurons having inhabitory D-1 receptors could contribute to the increase of sleep.
EMD 281014, a new selective serotonin 5-HT2A receptor antagonist.
TLDR
The 5-HT2A receptor ligand 7-[4-[2-(4-fluoro-phenyl)-ethyl]-piperazine-1-carbonyl]-1H-indole-3-carbonitrile HCl (EMD 281014) selectively binds to human (h) and rat 5- HT2A receptors, demonstrating unique selectivity and efficacy.
On the relationship of 5‐hydroxytryptamine neurons to 5‐hydroxytryptamine 2A receptor‐immunoreactive neuronal processes in the brain stem of rats. A double immunolabelling analysis
TLDR
The5-HT2A immunoreactivity demonstrated in the nerve terminal or dendritic-like structures of regions of the nucleus raphe pallidus, nucleus interfascicularis, motor nucleus of the trigeminal nerve, the ventral and dorsal tegmental nuclei and the median eminence by means of double immunofluorescence procedures were shown to be associated with 5-HT immunoreactive cell body-dendritic and/or nerve terminal structures.
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