The 5-HT2 Antagonist Ritanserin Decreases Sleep in Cats

Sommerfelt, Liv; Ursin, Reidun

doi:10.1093/sleep/16.1.15

Cited by 21 publications

(4 citation statements)

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“…Following ritanserin and deramciclane treatments, DS was slightly increased. The sleep inducing effect of ritanserin was reported earlier in rats (Dugovic and Wauquier, 1987;Vanderwolf 1988;Dugovic et al 1989;Walker et al 1989;Stutzmann et al 1992;Kirov and Moyanova, 1995), and humans (Vanderwolf 1984;Idzikowski et al 1986;Gruneis et al 1989), while the opposite effect was found in cats (Sommerfelt and Ursin, 1993). Deramciclane showed a similar synchronizing effect as ritanserin that was evident in the increase of total deep sleep, in the lengthening of sleep episodes and also in the more frequent occurrence of high voltage spindles compared to vehicle.…”

Section: Length Of Sleep Stagessupporting

confidence: 64%

Differential EEG effects of the anxiolytic drugs, deramciclane (EGIS-3886), ritanserin and chlordiazepoxide in rats

Détári¹,

Szentgyörgyi²,

Hajnik³

et al. 1999

Psychopharmacology

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The influence of serotonergic and benzodiazepine type anxiolytic drugs on the cortical activation and sleep-wakefulness cycle were compared by evaluating the effects of ritanserin and deramciclane (EGIS-3886), two 5-HT2 receptor antagonists, and chlordiazepoxide on the electroencephalogram (EEG) in freely moving rats. Following drug administration (1, 3, and 10 mg/kg, PO for all drugs), EEG was continuously sampled for 6 h and power spectra were calculated for every 5 s to assess changes in slow wave activity and sleep phases. In a separate test, anticonvulsant effects of the drugs were examined in mice. Both deramciclane and ritanserin slightly increased total time spent in deep sleep (DS) and lengthened sleep episodes. In contrast, chlordiazepoxide had a strong inhibitory action on DS, sleep time being shifted to more superficial light sleep (LS). The incidence and length of the high voltage spindle (HVS) episodes characteristic for the motionless, awake rat were increased at the highest dose of both deramciclane and ritanserin, while it was decreased by chlordiazepoxide. In mice, chlordiazepoxide had a marked anticonvulsant effect, while deramciclane was moderately effective and ritanserin ineffective. In conclusion, the 5-HT2 receptor antagonist anxiolytic drugs seem to be superior compared to the benzodiazepine type anxiolytic drug, chlordiazepoxide, as ritanserin and deramciclane improved sleep quality by increasing sleep episode length and time spent in DS, while chlordiazepoxide enhanced sleep fragmentation and decreased DS.

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Section: Length Of Sleep Stagessupporting

confidence: 64%

Differential EEG effects of the anxiolytic drugs, deramciclane (EGIS-3886), ritanserin and chlordiazepoxide in rats

Détári¹,

Szentgyörgyi²,

Hajnik³

et al. 1999

Psychopharmacology

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“…Interestingly, ritanserin has the opposite effect, decreasing slow-wave sleep in cats 38. The increase in slow-wave sleep caused by 5-HT 2 antagonists in rats appears to be more predictive of effects in humans than are the cat data (see below).…”

Section: -Ht2a Receptor Antagonists and Sleep In Animal Modelsmentioning

confidence: 95%

“… 34 – 37 Interestingly, ritanserin has the opposite effect, decreasing slow-wave sleep in cats. 38 The increase in slow-wave sleep caused by 5-HT 2 antagonists in rats appears to be more predictive of effects in humans than are the cat data (see below). Other 5-HT 2 receptor antagonists, such as Fananserin, pruvanserin, and nelotanserin, have shown increases in non-REM or slow-wave sleep in rats, 29 , 39 , 40 and eplivanserin and pruvanserin also show decreases in REM sleep in rats.…”

Section: -Ht 2a Receptor Antagonists and Sleep In Animal Modelsmentioning

confidence: 98%

Role of 5-HT2A receptor antagonists in the treatment of insomnia

Vanover¹,

Davis²

2010

NSS

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Insomnia encompasses a difficulty in falling asleep (sleep-onset insomnia) and/or a difficulty in staying asleep (SMI). Several selective serotonin-2A (5-HT 2A ) receptor antagonists have been in development as potential treatments for SMI. However, none have shown a sufficiently robust benefit-to-risk ratio, and none have reached market approval. We review the role of the 5-HT 2A mechanism in sleep, the preclinical and clinical data supporting a role for 5-HT 2A receptor antagonism in improving sleep maintenance, and the status of 5-HT 2A receptor antagonists in clinical development. Overall, the polysomnography data strongly support an increase in slow-wave sleep and a decrease in waking after sleep onset following treatment with 5-HT 2A receptor antagonists, although it has been more difficult to show subjective improvements in sleep with these agents. The incidence and prevalence of SMI, whether primary or secondary to psychiatric, neurologic, or other medical conditions, will increase as our population ages. There will be an increased need for safe and efficacious treatments of insomnia characterized by difficulty maintaining sleep, and there remains much promise for 5-HT 2A receptor antagonism to play a role in these future treatments.

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“…Furthermore, pharmacological studies provided evidence for a wake-promoting function of 5-HT (Monti, 2011). Blockade of 5-HT2 receptors promotes sleep in humans (Idzikowski et al, 1986) and rats (Dugovic and Wauquier, 1987), but increases wakefulness in cats (Sommerfelt and Ursin, 1993). By contrast, 5-HT was originally identified as a sleep-promoting neuromodulator since depletion of serotonin (Torda, 1967;Koella, 1968;Mouret et al, 1968), ablation (Jouvet, 1968(Jouvet, , 1972 or cooling (Cespuglio et al, 1976) of the raphe area produced transient insomnia.…”

Section: Introductionmentioning

confidence: 99%

Reciprocal lateral hypothalamic and raphé GABAergic projections promote wakefulness

Gazea

Furdan

Sere

et al. 2020

Preprint

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The lateral hypothalamus (LH), together with multiple neuromodulatory systems of the brain, such as the dorsal raphe nucleus (DR), is implicated in arousal, yet interactions between these systems are just beginning to be explored. Using a combination of viral tracing, circuit mapping, electrophysiological recordings from identified neurons and combinatorial optogenetics, we show that GABAergic neurons in the LH selectively inhibit GABAergic neurons in the DR resulting in disinhibition of a substantial fraction of its neurons that ultimately promotes arousal. These DR GABAergic neurons are wake active and project to multiple brain areas involved in the control of arousal including the LH, where their specific activation potently influences local network activity leading to arousal from sleep. Our results show how mutual inhibitory projections between the LH and the DR promote wakefulness through disinhibitory mechanisms and suggest a complex arousal control by intimate interactions between long-range connections and local circuit dynamics.

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The 5-HT2 Antagonist Ritanserin Decreases Sleep in Cats

Cited by 21 publications

References 0 publications

Differential EEG effects of the anxiolytic drugs, deramciclane (EGIS-3886), ritanserin and chlordiazepoxide in rats

Differential EEG effects of the anxiolytic drugs, deramciclane (EGIS-3886), ritanserin and chlordiazepoxide in rats

Role of 5-HT2A receptor antagonists in the treatment of insomnia

Reciprocal lateral hypothalamic and raphé GABAergic projections promote wakefulness

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