Effect of the histamine H3-antagonist clobenpropit on spatial memory deficits induced by MK-801 as evaluated by radial maze in Sprague–Dawley rats

Huang, Yu; Hu, Wei; Chen, Zhong; Zhang, Li san; Shen, Hai Qing; Timmerman, Henk; Leurs, Rob; Yanai, Kazuhiko

doi:10.1016/j.bbr.2003.09.002

Cited by 62 publications

(53 citation statements)

References 23 publications

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“…Thioperamide is highly potent at rat H 3 receptors with K i = 4.3 nM (Arrang et al, 1987a;Hill et al, 1997) that has been found broadly effective in vivo in a large number of behavioral models, including elevated plus maze learning, Morris water maze, Barnes maze (Miyazaki et al, 1995;Komater et al, 2005), and others. Clobenpropit (41) is likewise highly potent in vitro, with pA 2 = 9.92 in the guinea pig ileum assay (Eriks et al, 1992) and activity in vivo, e.g., in models of working memory, seizure, and Alzheimer's disease (Yokoyama et al, 1994;Zhang et al, 2003;Harada et al, 2004;Huang et al, 2004;Bardgett et al, 2011). Clobenpropit and thioperamide, however, also have potent activity at H 4 receptors (Lim et al, 2009), and thioperamide also is active at 5HT 3 receptors (Leurs et al, 1995b).…”

Section: E H 3 -Selective Ligandsmentioning

confidence: 99%

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

et al. 2015

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Section: E H 3 -Selective Ligandsmentioning

confidence: 99%

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

et al. 2015

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“…In the social memory [64,65], rats treated with H 3 R antagonists/inverse agonists performed better than controls in the five-trial inhibitory avoidance task [66,67] and the five-choice serial reactiontime test [68]. Further studies indicated that both imidazole and nonimidazole H 3 R antagonists/ inverse agonists exerted procognitive effects in cognitively impaired animals, as observed in senescence-accelerated mice or scopolamineimpaired rats challenged in a passive-avoidance response [69,70], scopolamine-impaired rats tested in object recognition [49,70,71] or the elevated plusmaze paradigm [72], and MK-801-treated rats evaluated in the radial maze [73]. Administration of nonimidazole H 3 R antagonists/inverse agonists, A-304121 or A-317920, improved cognitive performances in spontaneously hypertensive rat pups that were normotensive during early develop ment, but exhibited many cognitive impairments [66,67].…”

Section: Characteristics Of the H 3 Rmentioning

confidence: 99%

Histamine neuronal system as a therapeutic target for the treatment of cognitive disorders

Blandina¹,

Munari

Giannoni

et al. 2010

Future Neurol.

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Much has been learned over the past 20 years about the role of histamine as a neurotransmitter. This brief article attempts to evaluate the progress accomplished in this field, and discusses the therapeutic potential of the H3 receptor (H3R). All histaminergic neurons are localized in the tuberomammillary nucleus of the posterior hypothalamus and project to almost all regions of the CNS. Histamine exerts its effect via interaction with specific receptors (H1R, H2R, H3R and H4R). Antagonists of both H1R and H2R have been successful as blockbuster drugs for treating allergic conditions and gastric ulcers. H4R is still awaiting better functional characterization, but the H3R is an attractive target for potential therapies of CNS disorders. Indeed, considerable interest was raised by reports that pharmacological blockade of H3Rs exerted procognitive effects in a variety of animal tasks analyzing different types of memory. In addition, blockade of H3Rs increased wakefulness and reduced bodyweight in animal models. Such findings hint at the potential use of H3R antagonists/inverse agonists for the treatment of Alzheimer’s disease and other dementias, attention-deficit hyperactivity disorder, obesity and sleep disorders. As a result, an increasing number of H3R antagonists/inverse agonists progress through the clinic for the treatment of a variety of conditions, including attention-deficit hyperactivity disorder, cognitive disorders, narcolepsy and schizophrenia. Moreover, the use of H3R antagonists/inverse agonists that weaken traumatic memories may alleviate disorders such as post-traumatic stress syndrome, panic attacks, specific phobias and generalized anxiety. The use of H3R ligands for the treatment of neurodegenerative disorders is demonstrated in several studies, indicating a role of the histamine neurons and H3Rs in neuroprotection. Recently, direct evidence demonstrated that histaminergic neurons are organized into functionally distinct circuits, impinging on different brain regions, and displaying selective control mechanisms. This could imply independent functions of subsets of histaminergic neurons according to their respective origin and terminal projections. The possibility that H3Rs control only some of those functions implies that H3R-directed therapies may achieve selective effects, with minimal side effects, and this may increase the interest regarding this class of drugs.

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“…Histamine is involved in regulating cognitive behavior. For example, it facilitates memory retrieval deficits induced by aging, hippocampal lesions, and scopolamine, as determined through passive and active avoidance tasks and an 8-arm radial maze test for rats [8][9][10] . α-Fluoromethylhistidine, a selective histidine decarboxylase (HDC) inhibitor, induces significant memory deficits in an active avoidance task and the 8-arm radial maze in rats [11] .…”

Section: Introductionmentioning

confidence: 99%

Ameliorating effect of histamine on impairment of cued fear extinction induced by morphine withdrawal in histidine decarboxylase gene knockout mice

et al. 2010

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Aim: Histamine plays an important role in morphine addiction and memory-dependent behavior. However, little is known about the effect of histamine on the impairment of memory after morphine withdrawal. This study was designed to investigate the effect of histamine on memory impairment induced by morphine withdrawal in histidine decarboxylase knockout (HDC-KO) and wild-type (WT) mice. Methods: WT and HDC-KO mice were given subcutaneous morphine or saline twice daily for 5 consecutive days. The mice received a cued or contextual fear conditioning session 7 days after the last injection. During subsequent days, mice received 4 cued or contextual extinction sessions (one session per day). Western blot was used to assess extracellular signal-regulated kinase (ERK) phosphorylation in the amygdala and hippocampus. Results: Morphine withdrawal did not affect the acquisition of cued or contextual fear responses. It impaired cued but not contextual fear extinction. The acquisition of cued and contextual fear responses was accelerated in HDC-KO mice. Histamine deficiency aggravated the impairment of cued fear extinction induced by morphine withdrawal, whereas histamine (icv, 5 µg/mouse) reversed this effect. Morphine withdrawal decreased ERK phosphorylation in the amygdala after cued fear extinction, especially in HDC-KO mice. Conclusion: These results suggest that morphine withdrawal specifically impairs cued fear extinction and histamine ameliorates this impairment. Its action might be mediated by the modulation of ERK phosphorylation in the amygdala. Histamine should be explored for possible roles in the prevention or treatment of morphine abuse and relapse.

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Effect of the histamine H3-antagonist clobenpropit on spatial memory deficits induced by MK-801 as evaluated by radial maze in Sprague–Dawley rats

Cited by 62 publications

References 23 publications

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

Histamine neuronal system as a therapeutic target for the treatment of cognitive disorders

Ameliorating effect of histamine on impairment of cued fear extinction induced by morphine withdrawal in histidine decarboxylase gene knockout mice

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