Effects of selective activation of the 5-HT1B receptor with CP-94,253 on sleep and wakefulness in the rat

  title={Effects of selective activation of the 5-HT1B receptor with CP-94,253 on sleep and wakefulness in the rat},
  author={Jaime M. Monti and Daniela Monti and H{\'e}ctor Jantos and Ana Ponzoni},

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

Systemic administration of selective 5-HT2C agonists and nonselective 5- HT2A/2C receptor agonists has been shown to reduce slow wave sleep (SWS) and REM sleep and to augment W in laboratory animals.

Involvement of the 5-HT1A and the 5-HT1B receptor in the regulation of sleep and waking

Overall, most studies support the possibility that stimulation of postsynaptic 5-HT1A receptors, e.g., via systemic administration of a high dose of agonists increases wakefulness and decreases sleep and the mechanism by which 5- HT1B receptors affect state modulation remain elusive.

5-HT1A/1B Receptor-Mediated Effects of the Selective Serotonin Reuptake Inhibitor, Citalopram, on Sleep: Studies in 5-HT1A and 5-HT1B Knockout Mice

Data indicate that the action of the SSRI citalopram on sleep in the mouse is essentially mediated by 5-HT1A receptors, which provides further support to the clinical strategy of antidepressant augmentation by5- HT1A antagonists, because the latter would also counteract the direct sleep-inhibitory side-effects of SSRIs.

Key Role of 5-HT1B Receptors in the Regulation of Paradoxical Sleep as Evidenced in 5-HT1B Knock-Out Mice

Analysis of spontaneous sleep–waking cycles and the effects of 5-HT receptor ligands on sleep in knock-out (5-HT1B−/−) mice indicates that 5- HT1B receptors participate in the regulation of paradoxical sleep in the mouse.

The role of 5-HT1A and 5-HT1B receptors in MDMA self-administration

MDMA-stimulated serotonin (5-HT) release was negatively associated with acquisition of MDMA self-administration, and a neurotoxic 5-HT lesion reduced the latency to acquire self- Administration, suggesting that MDMA-produced 5- HT release is an important component of self-Administration.

Serotonin control of sleep-wake behavior.

  • J. Monti
  • Biology, Psychology
    Sleep medicine reviews
  • 2011



Effects of the selective 5‐HT1B agonist, CGS 12066B, on sleep/waking stages and EEG power spectrum in rats

The increase in waking together with a general deactivation suggest complex effects of CGS 12066B on the sleep/waking axis.

Functional activity of 5‐HT2 receptors in the modulation of the sleep/wakefulness states

Questions remain with regard to the physiological significance of the 5‐HT2 receptor‐mediated deep SWS regulation, the anatomical site(s) of 5‐ HT2 receptors involved in this regulation and the mechanism underlying diurnal fluctuations in the functional activity of 5-HT2 receptors.

Biochemical and behavioral studies of the 5‐HT1B receptor agonist, CP‐94,253

CP‐94,253, 3‐(1,2,5,6‐tetrahydro‐4‐pyridyl)‐5‐propoxypyrrolo[3,2‐b]pyridine, a new serotonergic ligand, was found to exhibit significantly greater binding affinity at 5‐HT1B receptors than at 5‐HT1A

Serotonin receptor subtypes : pharmacological significance and clinical implications

The 5-HT receptors modulate glutamate release in cerebellum and cholecystokinin release in nucleus accumbens and possible relevance to cerebellar ataxias and to anxiety, M. Raiteri et al serotonin and eating disorders - pharmacological relationships.

Functional correlates of serotonin 5-HT1 recognition sites.

  • D. Hoyer
  • Biology, Chemistry
    Journal of receptor research
  • 1988
It is shown that functional correlates do indeed exist for subtypes of 5-HT1 recognition sites; moreover, these are markedly different from the effects mediated by 5- HT2 (5-HT D) or 5 -HT3 (5 -HT M) receptors.

Dose‐dependent effects of the 5‐HT1A receptor agonist 8‐OH‐DPAT on sleep and wakefulness in the rat

SUMMARY  Sleep and wakefulness were studied in rats following administration of a selective 5‐HT1A agonist (8‐OH‐DPAT), a non‐selective 5‐HT1A antagonist [(‐) pindolol] and a combination of 8‐OH‐DPAT

Neuromédiateurs et facteurs hypnogènes.

The following hypothesis may solve contradictions: when 5HT neurons are active during waking, they initiate through neurohormonal mechanisms the biosynthesis of sleep factor(s) which are stored until they trigger sleep, and the amount of waking may be correlated with subsequent sleep.

A proposed new nomenclature for 5-HT receptors.