Effect of 5-HT2A/2B/2C receptor agonists and antagonists on sleep and waking in laboratory animals and humans

Kitka, Tamás; Bagdy, György

doi:10.1007/978-3-7643-8561-3_15

Cited by 4 publications

(1 citation statement)

References 71 publications

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“…The pD 2 value for the 5-HT 2B agonist BW723C86 found here is closer to the value found for 5-HT 2A receptor rather than for 5-HT 2B receptor (Kitka and Bagdy, 2008). The pK B value for the 5-HT 2B antagonist LY266097 we observed (ϳ8) is similar to the one reported in rat jugular vein (Audia et al, 1996), and it is closer to the pK B value of this antagonist toward 5-HT 2A receptor (7.7) rather than toward 5-HT 2B receptor (9.3) (Kitka and Bagdy, 2008). A contraction mediated by 5-HT 2B receptor activation was observed in aorta from hypertensive but not from normotensive rats (Russell et al, 2002).…”

Section: -Ht 2 Receptorssupporting

confidence: 83%

Serotonin Receptors in Rat Jugular Vein: Presence and Involvement in the Contraction

Linder

Gaskell

Szasz

et al. 2010

J Pharmacol Exp Ther

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Serotonin (5-hydroxytryptamine; 5-HT) is released during platelet aggregation, a phenomenon commonly observed in blood clot formation and venous diseases. Once released, 5-HT can interact with its receptors in the peripheral vasculature to modify vascular tone. The goal of this study was to perform a detailed pharmacological characterization of the 5-HT receptors involved in the contractile response of the rat jugular vein (RJV) using recently developed drugs with greater selectivity toward 5-HT receptor subtypes. We hypothesized that, as for other blood vessels, the 5-HT 1B/1D and 5-HT 2B receptor subtypes mediate contraction in RJV alongside the 5-HT 2A receptor subtype. Endothelium-intact RJV rings were set up in an isolated organ bath for isometric tension recordings, and contractile concentration-effect curves were obtained for 13 distinct serotonergic receptor agonists. Surprisingly, the 5-HT 1A and the mixed 5-HT 1A/1B receptor agonists (Ϯ)-2-dipropyl-amino-8-hydroxyl-1,2,3,4-tetrahydronapthalene (8-OH-DPAT) and 5-methoxy-3 (1,2,3,6-tetrahydropyridin-4-yl) (1H indole) (RU24969) caused contractions that were antagonized Serotonin (5-hydroxytryptamine; 5-HT) was first described as a substance with the ability to increase smooth muscle tone (Vialli and Erspamer, 1937;Rapport et al., 1948). 5-HT is synthesized by the enterochromaffin cells and released into the circulation. In the periphery, platelets are the largest store for 5-HT. It is interesting that our laboratory recently showed that peripheral vasculature has the ability to synthesize, take up, and metabolize 5-HT (Linder et al., 2008;. Moreover, the amount of 5-HT measured in veins is comparatively higher than in arteries, suggesting that peripheral veins also may constitute important stores of the amine (Linder et al., 2008). Thus, by controlling the amount of 5-HT within the peripheral vasculature environment, veins may exert relevant roles in adjusting vascular tone.

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Section: -Ht 2 Receptorssupporting

confidence: 83%

Serotonin Receptors in Rat Jugular Vein: Presence and Involvement in the Contraction

Linder

Gaskell

Szasz

et al. 2010

J Pharmacol Exp Ther

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The Role of 5-HT2A/2C Receptors in Sleep and Waking

Monti¹,

Jantos²

2010

5-Ht2c Receptors in the Pathophysiology of CNS Disease

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Chronic escitalopram treatment caused dissociative adaptation in serotonin (5-HT) 2C receptor antagonist-induced effects in REM sleep, wake and theta wave activity

et al. 2014

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Several multi-target drugs used in treating psychiatric disorders, such as antidepressants (e.g. agomelatine, trazodone, nefazodone, amitriptyline, mirtazapine, mianserin, fluoxetine) or most atypical antipsychotics, have 5-hydroxytryptamine 2C (5-HT2C) receptor-blocking property. Adaptive changes in 5-HT2C receptor-mediated functions are suggested to contribute to therapeutic effects of selective serotonin reuptake inhibitor (SSRI) antidepressants after weeks of treatment, at least in part. Beyond the mediation of anxiety and other functions, 5-HT2C receptors are involved in sleep regulation. Anxiety-related adaptive changes caused by antidepressants have been studied extensively, although sleep- and electroencephalography (EEG)-related functional studies are still lacking. The aim of this study was to investigate the effects of chronic SSRI treatment on 5-HT2C receptor antagonist-induced functions in different vigilance stages and on quantitative EEG (Q-EEG) spectra. Rats were treated with a single dose of the selective 5-HT2C receptor antagonist SB-242084 (1 mg/kg, i.p.) or vehicle at the beginning of passive phase following a 20-day-long SSRI (escitalopram; 10 mg/kg/day, osmotic minipump) or VEHICLE pretreatment. Fronto-parietal electroencephalogram, electromyogram and motility were recorded during the first 3 h of passive phase. We found that the chronic escitalopram pretreatment attenuated the SB-242084-caused suppression in rapid eye movement sleep (REMS). On the contrary, the 5-HT2C receptor antagonist-induced elevations in passive wake and theta (5-9 Hz) power density during active wake and REMS were not affected by the SSRI. In conclusion, attenuation in certain, but not all vigilance- and Q-EEG-related functions induced by the 5-HT2C receptor antagonist, suggests dissociation in 5-HT2C receptor adaptation.

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Effect of 5-HT2A/2B/2C receptor agonists and antagonists on sleep and waking in laboratory animals and humans

Cited by 4 publications

References 71 publications

Serotonin Receptors in Rat Jugular Vein: Presence and Involvement in the Contraction

Serotonin Receptors in Rat Jugular Vein: Presence and Involvement in the Contraction

The Role of 5-HT2A/2C Receptors in Sleep and Waking

Chronic escitalopram treatment caused dissociative adaptation in serotonin (5-HT) 2C receptor antagonist-induced effects in REM sleep, wake and theta wave activity

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