Functional activity of 5‐HT2receptors in the modulation of the sleep/wakefulness states

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Abstract
SUMMARY In the light of recent pharmacological investigations using agonists and antagonists that have potent actions on 5‐hydroxytryptamine‐2 (5‐HT2) receptors, the possible functional role of 5‐HT2receptors in the modulation of the sleep/wakefulness states was examined. Data obtained from animals and from clinical studies suggest that serotonin may exert an inhibitory control on deep slow‐wave sleep (SWS) through 5‐HT2receptors. In further investigations, the existence of a diurnal variation in the functional activity of 5‐HT2receptors, that depends on the day/night cycle and/or the melatonin rhythm, was revealed. Questions remain with regard to the physiological significance of the 5‐HT2receptor‐mediated deep SWS regulation, the anatomical site(s) of 5‐HT2receptors involved in this regulation and the mechanism underlying diurnal fluctuations in the functional activity of 5‐HT2receptors.