Regular paperEffects of selective activation or blockade of the histamine H3 receptor on sleep and wakefulness☆
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Neuroprotective effect of histamine H3 receptor blockade on methamphetamine-induced cognitive impairment in mice
2023, Pharmacology Biochemistry and BehaviorCitation Excerpt :Since histamine's central actions largely depend upon the actions of H3R, H3R is considered a promising target for a wide spectrum of central nervous system disorders (Gemkow et al., 2009). THIO is one of the most widely used H3R antagonists (Masini et al., 2017), which can freely pass blood-brain barrier to inhibit the release of histamine (Monti et al., 1991). THIO has a very low affinity for H1 and H2 receptors and shows potent activity both in vivo and in vitro (Arrang et al., 1987).
Effects of propofol on sleep architecture and sleep–wake systems in rats
2021, Behavioural Brain ResearchHistamine may contribute to vortioxetine's procognitive effects; possibly through an orexigenic mechanism
2016, Progress in Neuro-Psychopharmacology and Biological PsychiatryReview of the histamine system and the clinical effects of H<inf>1</inf> antagonists: Basis for a new model for understanding the effects of insomnia medications
2013, Sleep Medicine ReviewsCitation Excerpt :As such, it would be expected that agents with H3 agonist effects have the potential to be useful for promoting sleep. In this regard there is evidence that the H3 receptor agonist R-α-methylhistamine injected into the region of the TM nucleus increases non-rapid eye movement (REM) sleep, and decreases wakefulness.39 The H3 receptor is also expressed in various brain regions including the cortex, hippocampus, amygdala, and brainstem where it functions as a heteroreceptor that plays a role in regulating release of other neurotransmitters, such as norepinephrine, glutamate, acetylcholine, and GABA.40
Histamine in the regulation of wakefulness
2011, Sleep Medicine ReviewsCitation Excerpt :In contrast, bilateral application of (R)-α-methyl-histamine into the TMN region promotes NREM sleep with a concomitant decrease in wakefulness and REM sleep suggesting that activation of H3 receptor in the TMN is likely to block histamine release resulting in reduced wakefulness. The NREM inducing effect of (R)-α-methyl-histamine is attenuated if the rats were pretreated with thioperamide.59 Oral administration of BP 2.94 (20–30 mg/kg) produces a dose-dependent increase in NREM sleep without affecting wakefulness or REM sleep in rats.
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Preliminary results presented at the 10th Congress of the European Sleep Research Society, Strasbourg (Monti et al., 1990).