The effects of zimeldine and alaproclate combined with a small dose of 5-HTP on waking and sleep stages in cats

Sommerfelt, Liv; Ursin, Reidun

doi:10.1016/0166-4328(87)90031-3

Cited by 16 publications

(2 citation statements)

References 29 publications

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“…This fmding is consistent with studies of 5-HT reuptake blockers (Sommerfelt and Ursin 1987) that typically demonstrate increased tonus associated with arousal, which we did not observe with eltoprazine. We suspect that circulat ing levels of eltoprazine result in a persistent inhibition of the pontine locus coeruleus alpha region (Sakai et al 1981), thus maintaining EMG tonus at higher levels during all phases of sleep than in physiologically nor mal sleep.…”

Section: Discussionsupporting

confidence: 92%

Dose-Related Suppression of REM Sleep and PGO Waves by the Serotonin-1 Agonist Eltoprazine

Quattrochi

Mamelak

Binder

et al. 1993

Neuropsychopharmacol

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Parenteral administration of the serotonin-1 agonist eltoprazine (0.0625 to 4.0 mglkg [0.0002 to 0.016 mmollkgJ) in freely moving cats produced significant suppression of electrophysiologic rapid eye movement (REM) sleep signs, ponto-geniculo-occipital (PGG) activity, and REM sleep behavior. The virtual total suppression of REM sleep (0.4%, 4.0 mglkg) and PGG wave activity (2 to 4 mglkg) in exchange for increasing amounts of non-REM (NREM) slow-wave sleep was a dose-dependent function of the amount of eltoprazine KEY WORDS: REM sleep; PGG waves; Serotonin; Eltoprazine Despite the large number of studies implicating sero tonin (5-HT) in the modulation of behavioral state, its exact role in the regulation of sleep and waking remains unclear. Pharmacological studies designed to elucidate the mechanism by which 5-HT neurotransmission aff ects behavioral state have reported paradoxical or contradictory results. While the listing of multiple 5-HT receptor subtypes (Glennon 1986;Peroutka 1988) has elucidated many of the pharmacological properties of ser otonin and underscores the complexity of its modula tory influences, this research has failed to provide a detailed understanding of behavioral state control and administered. Wakefulness was unaffected by eltoprazine regardless of dose. Concurrent with this dose-dependent suppression of REM was a dose-dependent increase in electroencephalographic synchrony and mean electromyographic amplitude. Since eltoprazine was found to shift the balance between REM and NREM sleep but did not change the balance between sleep and waking, it is a potentially useful tool for the investigation of serotonergic-cholinergic interaction.lNeuropsychopharmacology 8:7-13, 1993J neurophysiological phenomena. One reason for this failure is that surprisingly few studies have focused on how administration of receptor-specifIc 5-HT agonists affects sleep, particularly rapid eye movement (REM) sleep.We have previously observed suppression of REM sleep by the parenteral administration of the 5-HTl agonist eltoprazine (Quattrochi et al. 1990) and docu mented the REM rebound that followed discontinua tion of the drug. These findings support the hypothe sis that REM sleep is under the inhibitory control of serotonin (Hobson and Steriade 1986). We now dem onstrate that the suppression of REM sleep is dose de pendent and show that the dose-response properties of one relatively specifIc REM sleep sign, ponto geniculo-occipital (PGO) waves, are quantitatively sen sitive to eltoprazine.PGO waves are of particular interest because they are highly specifIc phenomena of REM sleep. Early studies by Jouvet (1969), Delorme et al. (1965), and De ment et al. (1973) indicated that PGO activity was sus ceptible to serotonergic inhibition; successive studies

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Section: Discussionsupporting

confidence: 92%

Dose-Related Suppression of REM Sleep and PGO Waves by the Serotonin-1 Agonist Eltoprazine

Quattrochi

Mamelak

Binder

et al. 1993

Neuropsychopharmacol

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“…Nevertheless, 5-HT can also contribute to increase sleep propensity, as first observations showed that either lesions of 5-HT neurons of the raphe system or inhibition of 5-HT synthesis induce a severe insomnia which could be reversed by restoring 5-HT synthesis (Jouvet 1999). Importantly, enhancing 5-HT tone by systemic administration of selective serotonin reuptake inhibitors (SSRIs) has been repeatedly reported to inhibit REM sleep across species (Slater et al 1978;Sommerfelt and Ursin 1987;Maudhuit et al 1994;Monaca et al 2003). Thus, upon the different approaches used, while 5-HT was first believed to be a neuromodulator of sleep, it is now further thought to promote cortical activation while impeding REM sleep onset during wake.…”

Section: 4mentioning

confidence: 99%

Pharmacosynthetic Deconstruction of Sleep-Wake Circuits in the Brain

Varin¹,

Bonnavion²

2018

Sleep-Wake Neurobiology and Pharmacology

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Changing concepts on the role of serotonin in the regulation of sleep and waking

Ursin¹

Serotonin and Sleep: Molecular, Functional and Clinical Aspects

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The effects of zimeldine and alaproclate combined with a small dose of 5-HTP on waking and sleep stages in cats

Cited by 16 publications

References 29 publications

Dose-Related Suppression of REM Sleep and PGO Waves by the Serotonin-1 Agonist Eltoprazine

Dose-Related Suppression of REM Sleep and PGO Waves by the Serotonin-1 Agonist Eltoprazine

Pharmacosynthetic Deconstruction of Sleep-Wake Circuits in the Brain

Changing concepts on the role of serotonin in the regulation of sleep and waking

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