Sleep and Waking during Acute Histamine H3 Agonist BP 2.94 or H3 Antagonist Carboperamide (MR 16155) Administration in Rats

Monti, Jaime M.; Jantos, Héctor; Ponzoni, Ana; Monti, Daniel

doi:10.1016/0893-133x(95)00151-3

Cited by 51 publications

(23 citation statements)

References 18 publications

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“…Radioligand competition studies using rat cortical membrane have demonstrated high affinity for the H 3 R antagonists, including ciproxifan, thioperamide, GSK189254 and ABT-239 (Arrang et al, 1987;Fox et al, 2005;Medhurst et al, 2007a;Monti et al, 1996).…”

Section: Discussionmentioning

confidence: 99%

Detection of low level histamine H3 receptor occupancy by autoradiography

Le¹,

Finn²,

Larijani³

et al. 2009

Journal of Neuroscience Methods

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Section: Discussionmentioning

confidence: 99%

Detection of low level histamine H3 receptor occupancy by autoradiography

Le¹,

Finn²,

Larijani³

et al. 2009

Journal of Neuroscience Methods

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“…The genetic disruption or pharmacological inhibition of HDC in mice results in a deficit in controlling wakefulness (33). Moreover, several H3R agonists, including imetit, although still controversial, increase slow-wave sleep by inhibiting histamine release (34)(35)(36). Thus, it might be argued that the anorexigenic effects of imetit might be due to this hypnotic action.…”

Section: Discussionmentioning

confidence: 99%

Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus

Yoshimoto

Miyamoto

Shimamura

et al. 2006

Proc. Natl. Acad. Sci. U.S.A.

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Histamine H3 receptors (H3Rs) are located on the presynaptic membranes and cell soma of histamine neurons, where they negatively regulate the synthesis and release of histamine. In addition, H3Rs are also located on nonhistaminergic neurons, acting as heteroreceptors to regulate the releases of other amines such as dopamine, serotonin, and norepinephrine. The present study investigated the effects of H3R ligands on appetite and body-weight regulation by using WT and H3R-deficient mice (H3RKO), because brain histamine plays a pivotal role in energy homeostasis. The results showed that thioperamide, an H3R inverse agonist, increases, whereas imetit, an H3R agonist, decreases appetite and body weight in diet-induced obese (DiO) WT mice. Moreover, in DiO WT mice, but not in DiO H3RKO mice, imetit reduced fat mass, plasma concentrations of leptin and insulin, and hepatic triglyceride content. The anorexigenic effects of imetit were associated with a reduction in histamine release, but a comparable reduction in histamine release with ␣-fluoromethylhistidine, an inhibitor of histamine synthesis, increased appetite. Moreover, the anorexigenic effects of imetit were independent of the melanocortin system, because imetit comparably reduced appetite in melanocortin 3 and 4 receptor-deficient mice. The results provide roles of H3Rs in energy homeostasis and suggest a therapeutic potential for H3R agonists in the treatment of obesity and diabetes mellitus.autoreceptor ͉ heteroreceptor ͉ appetite regulation O besity has recently become a matter of great concern, because it is considered one of the highest risk factors for diabetes mellitus, hyperlipidemia, and arteriosclerosis. To maintain body weight, caloric intake and energy expenditure must be balanced, and excessive caloric intake is a leading cause of obesity (1). There is growing evidence that the brain receives and integrates information related to energy status from peripheral tissues and that appetite is under the control of numerous neurotransmitters and hormones, such as neuropeptide Y, melanocortin, leptin, and ghrelin (2, 3)Histamine is a classical inflammatory mediator in peripheral tissues and also functions as a neurotransmitter in the brain. Histamine plays a pivotal role in various physiological functions, such as feeding behavior and energy homeostasis (4). Intracerebroventricular administration of histamine consistently decreases appetite in several species (4). Mice with genes disrupted for histamine H1 receptor or histidine decarboxylase (HDC), a ratelimiting enzyme for histamine synthesis, are prone to becoming obese on a high-fat diet or at advanced age (5-8). Furthermore, several antipsychotic drugs with high affinities for H1 receptors are known to cause weight gain in rodents and humans (9). These results suggest a significant role for histamine and H1 receptors in feeding behavior and body-weight regulation.Histamine H3 receptors (H3Rs) were pharmacologically identified more than a decade ago and recently cloned (10, 11). They are predominantly ex...

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“…Several H3-antagonists are being developed and have been reported to effect wakefulness and cognition in rodents [52,62,63]. In addition, enhanced performance was demonstrated in animal models for ADHD [64,65].…”

Section: Discussionmentioning

confidence: 98%

“…Although the increased wakefulness following administration of an H3-antagonist can be the result of increased histamine levels, Monti et al, (1996) [52] already noted that the noradrenaline, dopamine, serotonin and acetylcholine neurotransmitter systems might also be involved, since H3-receptors are also heteroreceptors. These receptors have indeed been shown to regulate release of dopamine, noradrenaline, serotonin and acetylcholine [53,54].…”

Section: H3-antagonismmentioning

confidence: 98%

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Stimulating Effects of H1-Antagonists

Theunissen

Vermeeren²,

Vuurman³

et al. 2006

CPD

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Whereas antihistamines are generally known for their sedative side effects, this review shows that several studies also found mild stimulating effects on performance for the H1-antagonists terfenadine, ebastine, fexofenadine and desloratadine. These stimulating effects were mostly demonstrated in tasks involving high levels of attention, e.g. divided attention tasks, vigilance tasks and driving tasks. The stimulating effects of these antihistamines were often dependent of the given dose; however the relation was not always linear. The mechanism responsible for the stimulating effects of these four antihistamines is still unclear, though it is hypothesized that it involves other neurotransmitters like dopamine and GABA, or that it acts through the H3 histamine receptor. Further research is needed to clarify the ambiguous role of histamine in processes of arousal. In addition, it would be useful to determine whether terfenadine, ebastine, fexofenadine and desloratadine can return allergic patient's performance back to their preclinical level.

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Sleep and Waking during Acute Histamine H3 Agonist BP 2.94 or H3 Antagonist Carboperamide (MR 16155) Administration in Rats

Cited by 51 publications

References 18 publications

Detection of low level histamine H3 receptor occupancy by autoradiography

Detection of low level histamine H3 receptor occupancy by autoradiography

Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus

Stimulating Effects of H1-Antagonists

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