Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic

Yokoyama, Fumikazu; Yamauchi, Miki; Oyama, Masayo; Okuma, Kunihiro; Onozawa, Kaname; Nagayama, Takako; Shinei, Rie; Ishikawa, Makoto; Suzuki, Yasuo; Kakui, Nobukazu

doi:10.1007/s00213-009-1528-1

Cited by 31 publications

(26 citation statements)

References 54 publications

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“…Moreover, the antidepressant-like behaviors observed for ST-1283 in the mouse TST, NSF, and FST were also blocked following administration of RAMH 10 mg/kg. Importantly, previous studies have shown that RAMH and immepip dihydrobromide, both H 3 R agonists, do not affect spontaneous locomotor activity, even at doses much higher than those in the pharmacologically effective range, suggesting that these H 3 agonists do not induce hypolocomotion, which may result from suppression of histaminergic neurotransmission 36,37. Moreover, previous studies have shown that anxiolytic drugs such as diazepam and buspirone (a serotonin 5-HT1A agonist) significantly inhibit brain histamine turnover in rodents 38,39.…”

Section: Discussionmentioning

confidence: 99%

Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H3 receptor antagonist ST-1283

Bahí¹,

Schwed²,

Walter³

et al. 2014

DDDT

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Previous studies have suggested a potential link between histamine H3 receptors (H3R) signaling and anxiolytic-like and antidepressant-like effects. The aim of this study was to investigate the acute effects of ST-1283, a novel H3R antagonist, on anxiety-related and depression-related behaviors in comparison with those of diazepam and fluoxetine. The effects of ST-1283 were evaluated using the elevated plus maze test, open field test, marbles burying test, tail suspension test, novelty suppressed feeding test, and forced swim test in male C57BL/6 mice. The results showed that, like diazepam, ST-1283 (7.5 mg/kg) significantly modified all the parameters observed in the elevated plus maze test. In addition, ST-1283 significantly increased the amount of time spent in the center of the arena without altering general motor activity in the open field test. In the same vein, ST-1283 reduced the number of buried marbles as well as time spent digging in the marbles burying test. The tail suspension test and forced swim test showed that ST-1283 was able to reduce immobility time, like the recognized antidepressant drug fluoxetine. In the novelty suppressed feeding test, treatment with ST-1283 decreased latency to feed with no effect on food intake in the home cage. Importantly, pretreatment with the H3R agonist R-α-methylhistamine abrogated the anxiolytic and antidepressant effects of ST-1283. Taken together, the present series of studies demonstrates the novel effects of this newly synthesized H3R antagonist in a number of preclinical models of psychiatric disorders and highlights the histaminergic system as a potential therapeutic target for the treatment of anxiety-related and depression-related disorders.

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Section: Discussionmentioning

confidence: 99%

Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H3 receptor antagonist ST-1283

Bahí¹,

Schwed²,

Walter³

et al. 2014

DDDT

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“…As indicated in the introduction, the effects of systemic histaminergic compounds on reconsolidation have not been examined to date. In a study examining retrieval, that is thought to share some functional features with reconsolidation, H 3 receptor agonists injected prior to the retention test of a contextually conditioned fear response were found to deteriorate memory performance, an interference that was readily prevented by thioperamide (Yokoyama et al, 2009). The inefficacy of thioperamide on reconsolidation contrasts with the facilitation that many H 3 receptor inverse agonists typically exert not only on consolidation but also on acquisition and retrieval of aversively, positively and non-reinforced tasks in mice and rats (Meguro et al, 1995;Ghi et al, 1998;Yates et al, 1999;Fox et al, 2003Fox et al, , 2005Esbenshade et al, 2005;Komater et al, 2005;Ligneau et al, 2007;Brioni et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Differential effects of histamine H3 receptor inverse agonist thioperamide, given alone or in combination with the N-methyl-d-aspartate receptor antagonist dizocilpine, on reconsolidation and consolidation of a contextual fear memory in mice

Charlier

Tirelli

2011

Neuroscience

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Abstract-Albeit there is no doubt that histamine and its H 3 receptors participate in several aspects of learning and memory, such as memory consolidation, nothing is known about their potential involvement in memory reconsolidation. On the basis of previous reports of pro-cognitive effects of histamine H 3 receptor inverse agonists (which augment histamine release), we investigated to what extent the most representative of them, thioperamide, is able to facilitate reconsolidation of a contextually-conditioned fear memory in C57BL/6J mice. We also examined the effects of thioperamide on the stark disruptive effect that the non-competitive N-methyl-D-aspartate (NMDA) antagonist dizocilpine (MK-801) typically exerts on both reconsolidation and consolidation. Post-training systemic injections (i.p.) of thioperamide facilitated consolidation at 10 and 20 mg/kg and reversed amnesia induced by an i.p. injection of 0.12 mg/kg dizocilpine at 5, 10 and 20 mg/kg. Importantly, none of the five thioperamide doses (2.5, 5, 10, 20 and 30 mg/kg) given right after reactivation (reexposure to the context in which training took place 48 h earlier) affected reconsolidation, whereas all similarly given doses of dizocilpine (0.03, 0.06 and 0.12 mg/kg) disrupted it more or less equally. By contrast, thioperamide was able to unambiguously reverse the deficit in reconsolidation induced by 0.12 mg/kg dizocilpine at 10 and 20, but not 5 mg/kg. This is the first demonstration of an involvement of the interactive articulation between histamine and NMDA receptors in the mechanisms of memory reconsolidation, which seems to be indifferent to an increase of brain histamine per se. The results suggest a qualitatively different participation of histaminergic signalling in the mechanisms of reconsolidation and consolidation. The precise circuits within which these interactions take place are yet to be identified.

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“…In contrast to the antagonists/inverse agonists, the H 3 receptor agonist imetit enhances sleep and dose-dependently attenuates ciproxifan-induced waking in mice, indicating that the effects of both ligands are mediated by H 3 receptors (Parmentier et al, 2007). Unlike the procognitive activity of antagonists, H 3 receptor agonists seem to possess anxiolytic-like profiles (Yokoyama et al, 2009) and thus would be expected to improve sleep after stress.…”

Section: H 3 Receptors: Targets For Arousal Control and Treatment Of mentioning

confidence: 99%

Histamine H₃ Receptors and Sleep-Wake Regulation

Lin

Sergeeva²,

Haas³

2010

J Pharmacol Exp Ther

119

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The histaminergic system fulfills a major role in the maintenance of waking. Histaminergic neurons are located exclusively in the posterior hypothalamus from where they project to most areas of the central nervous system. The histamine H 3 receptors are autoreceptors damping histamine synthesis, the firing frequency of histamine neurons, and the release of histamine from axonal varicosities. It is noteworthy that this action also extends to heteroreceptors on the axons of most other neurotransmitter systems, allowing a powerful control over multiple homeostatic functions. The particular properties and locations of histamine H 3 receptors provide quite favorable attributes to make this a most promising target for pharmacological interventions of sleep and waking disorders associated with narcolepsy, Parkinson's disease, and other neuropsychiatric indications. Sleep and WakingWakefulness and consciousness depend on perturbation of intrinsic cortical activity that is achieved through ascending activating systems taking a ventral route, the ascending reticular activating system of Moruzzi and Magoun, and a dorsal route whose main station is the hypothalamus. Both pathways send direct projections to the cortex and indirect ones through the thalamus, the door to perception of sensory input. Both waking and paradoxical sleep (REM) are conscious states and need activation by subcortical structures, although in different ways.Cholinergic neurons of the brainstem and the basal forebrain discharge tonically during both wakefulness and paradoxical sleep, can directly excite cortical neurons, and facilitate the thalamo-cortical transmission by inhibiting the thalamic reticular sleep-onset generator. Brainstem and basal forebrain cholinergic neurons are excited by glutamatergic, noradrenergic, and histaminergic neurons; they are particularly important in cortical electroencephalogram arousal, but do not seem to be essential for the waking state (Szymusiak and McGinty, 1986;Lin, 2000).Monoaminergic ascending projections containing catecholamines and serotonin are involved in sleep-waking regulation and the pathophysiology of major psychiatric disorders, schizophrenia, and depression, all of which include disturbance in sleep-waking. Inhibition of catecholamine synthesis decreases waking, and psychostimulants, such as amphetamine, increase waking through accumulation of catecholamines. A lesion of the serotonergic dorsal raphe causes insomnia. These aminergic systems mediate different behavioral expressions during waking, activate immediate early genes, and facilitate locomotion, perception, and cognition (reviewed in Jones, 2005).

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Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic

Cited by 31 publications

References 54 publications

Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H3 receptor antagonist ST-1283

Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H3 receptor antagonist ST-1283

Differential effects of histamine H3 receptor inverse agonist thioperamide, given alone or in combination with the N-methyl-d-aspartate receptor antagonist dizocilpine, on reconsolidation and consolidation of a contextual fear memory in mice

Histamine H₃ Receptors and Sleep-Wake Regulation

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Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic

Cited by 31 publications

References 54 publications

Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H3 receptor antagonist ST-1283

Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H3 receptor antagonist ST-1283

Differential effects of histamine H3 receptor inverse agonist thioperamide, given alone or in combination with the N-methyl-d-aspartate receptor antagonist dizocilpine, on reconsolidation and consolidation of a contextual fear memory in mice

Histamine H3 Receptors and Sleep-Wake Regulation

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Histamine H₃ Receptors and Sleep-Wake Regulation