Acetylcholine, Histamine, and Cognition: Two Sides of the Same Coin

Blandina, Patrizio; Efoudebe, Marcel; Cenni, Gabriele; Mannaioni, P. F.; Passani, Maria Beatrice

doi:10.1101/lm.68004

Cited by 74 publications

(51 citation statements)

References 123 publications

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“…Similarly to clozapine, functional improvement of the prefrontal cortex was also perhaps mediated in part by the effects of pyrilamine on freezing time. It has been shown that an increase in endogenous histamine decreased the mnemonic ability in the acoustic fear conditioning test through inhibiting acetylcholine release (31). The blockade of H 1 receptor by pyrilamine may abolish this effect of endogenous histamine.…”

Section: Discussionmentioning

confidence: 99%

Blocking Histamine H1 Improves Learning and Mnemonic Dysfunction in Mice With Social Isolation Plus Repeated Methamphetamine Injection

et al. 2008

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Abstract. The aim of this study was to investigate the effects of histamine H 1 and H 3 antagonists on learning and mnemonic dysfunction in mice. Two H 1 antagonists, pyrilamine and clozapine, and the prototypic H 3 antagonist thioperamide were used to study the role of histamine in mice with social isolation and repeated methamphetamine administration. Mice with social isolation and repeated methamphetamine administration showed significant disruption of prepulse inhibition as compared to both the socially-housed mice and isolation-housing mice. Furthermore, social isolation and repeated methamphetamine administration caused significant learning and mnemonic dysfunctions. Treatment with clozapine improved learning and mnemonic ability in all of the tasks. Pyrilamine treatment ameliorated performance in all the tests examined except for the passive avoidance test. Thioperamide, however, did not change the learning and mnemonic ability. Donepezil, an acetylcholinesterase inhibitor, reversed the learning and mnemonic dysfunction in all four tasks. The present study has shown that blockade of histamine H 1 receptor improved the learning and mnemonic ability in mice, raising the possibility that treatment with clozapine or pyrilamine may improve learning and mnemonic performance in certain patients with psychiatric diseases such as schizophrenic patients with cognitive dysfunction.

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Section: Discussionmentioning

confidence: 99%

Blocking Histamine H1 Improves Learning and Mnemonic Dysfunction in Mice With Social Isolation Plus Repeated Methamphetamine Injection

et al. 2008

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“…Histamine is a neurotransmitter that is associated with memory and attentional processes, and its effects on these processes might be mediated in part through cross-talk with the cholinergic system (Philippu and Prast, 2001;Blandina et al, 2004). For example, histaminergic afferents to cholinergic cell bodies in the basal forebrain help to increase ACh release at cholinergic terminals in the PFC and hippocampus (Cecchi et al, 2001;Bacciottini et al, 2002).…”

Section: Discussionmentioning

confidence: 99%

The 5-Hydroxytryptamine₄ Receptor Agonists Prucalopride and PRX-03140 Increase Acetylcholine and Histamine Levels in the Rat Prefrontal Cortex and the Power of Stimulated Hippocampal θ Oscillations

Johnson

Drummond²,

Grimwood³

et al. 2012

J Pharmacol Exp Ther

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5-Hydroxytryptamine (5-HT) 4 receptor agonists reportedly stimulate brain acetylcholine (ACh) release, a property that might provide a new pharmacological approach for treating cognitive deficits associated with Alzheimer's disease. The purpose of this study was to compare the binding affinities, functional activities, and effects on neuropharmacological responses associated with cognition of two highly selective 5-HT 4 receptor agonists, prucalopride and 6,7-dihydro-4-hydroxy-7-isopropyl-6-oxo-N-[3-(piperidin-1-yl)propyl]thieno[2,3-b]pyridine-5-carboxamide (PRX-03140). In vitro, prucalopride and PRX-03140 bound to native rat brain 5-HT 4 receptors with K i values of 30 nM and 110 nM, respectively, and increased cAMP production in human embryonic kidney-293 cells expressing recombinant rat 5-HT 4 receptors. In vivo receptor occupancy studies established that prucalopride and PRX-03140 were able to penetrate the brain and bound to 5-HT 4 receptors in rat brain, achieving 50% receptor occupancy at free brain exposures of 330 nM and 130 nM, respectively. Rat microdialysis studies revealed that prucalopride maximally increased ACh and histamine levels in the prefrontal cortex at 5 and 10 mg/kg, whereas PRX-03140 significantly increased cortical histamine levels at 50 mg/kg, failing to affect ACh release at doses lower than 150 mg/kg. In combination studies, donepezil-induced increases in cortical ACh levels were potentiated by prucalopride and PRX-03140. Electrophysiological studies in rats demonstrated that both compounds increased the power of brainstem-stimulated hippocampal oscillations at 5.6 mg/kg. These findings show for the first time that the 5-HT 4 receptor agonists prucalopride and PRX-03140 can increase cortical ACh and histamine levels, augment donepezil-induced ACh increases, and increase stimulated-hippocampal power, all neuropharmacological parameters consistent with potential positive effects on cognitive processes.

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“…It is known that manipulation of the histaminergic central system during several learning paradigms modifies animal behavior; however, the results are often contradictory, as both facilitatory and inhibitory effects of histamine on memory have been described (see review [23]). This is not too surprising, as memory is a complex process that consists of related but dissociable events, involving, in the elaboration of disparate learning situations, distinct brain regions activated to different degrees and at different times.…”

mentioning

confidence: 99%

“…We proposed that the controversial role of histamine can be partially reconciled with the observation that histamine modulates the cholinergic function differently in discrete brain regions that are known to be devoted to the acquisition and/or expression of specific behaviors [23,24]. In our laboratory, we are interested in emotional memory, which we study using an adversely motivated training task, contextual fear conditioning.…”

mentioning

confidence: 99%

Histamine in the brain: Beyond sleep and memory

Passani¹,

Giannoni²,

Bucherelli

et al. 2007

Biochemical Pharmacology

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Acetylcholine, Histamine, and Cognition: Two Sides of the Same Coin

Cited by 74 publications

References 123 publications

Blocking Histamine H1 Improves Learning and Mnemonic Dysfunction in Mice With Social Isolation Plus Repeated Methamphetamine Injection

Blocking Histamine H1 Improves Learning and Mnemonic Dysfunction in Mice With Social Isolation Plus Repeated Methamphetamine Injection

The 5-Hydroxytryptamine₄ Receptor Agonists Prucalopride and PRX-03140 Increase Acetylcholine and Histamine Levels in the Rat Prefrontal Cortex and the Power of Stimulated Hippocampal θ Oscillations

Histamine in the brain: Beyond sleep and memory

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Acetylcholine, Histamine, and Cognition: Two Sides of the Same Coin

Cited by 74 publications

References 123 publications

Blocking Histamine H1 Improves Learning and Mnemonic Dysfunction in Mice With Social Isolation Plus Repeated Methamphetamine Injection

Blocking Histamine H1 Improves Learning and Mnemonic Dysfunction in Mice With Social Isolation Plus Repeated Methamphetamine Injection

The 5-Hydroxytryptamine4 Receptor Agonists Prucalopride and PRX-03140 Increase Acetylcholine and Histamine Levels in the Rat Prefrontal Cortex and the Power of Stimulated Hippocampal θ Oscillations

Histamine in the brain: Beyond sleep and memory

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Product

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The 5-Hydroxytryptamine₄ Receptor Agonists Prucalopride and PRX-03140 Increase Acetylcholine and Histamine Levels in the Rat Prefrontal Cortex and the Power of Stimulated Hippocampal θ Oscillations