Antihistaminic drugs increase feeding, while histidine suppresses feeding in rats

Orthen-Gambill, Nilla

doi:10.1016/0091-3057(88)90315-2

Cited by 70 publications

(34 citation statements)

References 19 publications

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“…Our findings predict that H1R-deleted mice should be resistant to the orexigenic actions of AAPDs and that H1 antihistamines should be orexigenic. In rats (35) and humans (36), H1 antihistamines have been reported to be orexigenic. Because these drugs typically are used sporadically and in substantially lower doses than AAPDs, effects on weight are less prominent for H1 antihistamines.…”

Section: Discussionmentioning

confidence: 99%

Antipsychotic drug-induced weight gain mediated by histamine H₁receptor-linked activation of hypothalamic AMP-kinase

Kim

Huang

Snowman

et al. 2007

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

359

253

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The atypical antipsychotic drugs (AAPDs) have markedly enhanced the treatment of schizophrenias but their use has been hindered by the major weight gain elicited by some AAPDs. We report that orexigenic AAPDs potently and selectively activate hypothalamic AMP-kinase, an action abolished in mice with deletion of histamine H1 receptors. These findings may afford a means of developing more effective therapeutic agents and provide insight into the hypothalamic regulation of food intake.atypical antipsychotic drugs ͉ obesity ͉ hypothalamus

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Section: Discussionmentioning

confidence: 99%

Antipsychotic drug-induced weight gain mediated by histamine H₁receptor-linked activation of hypothalamic AMP-kinase

Kim

Huang

Snowman

et al. 2007

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

359

253

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“…Intraperitoneal injection of L-histidine, had the same effect as histamine in reducing food intake. [11][12][13] Administration of metoprine, an enzyme that blocks histamine breakdown, suppresses food intake in rats. 14,15 a-Fluoromethylhistidine is a specific and irreversible inhibitor of the histidine decarboxylase enzyme and has the ability to deplete histamine from the brain neurons.…”

Section: Introductionmentioning

confidence: 99%

Effect of histaminergic manipulation on weight in obese adults: a randomized placebo controlled trial

Barak¹,

Greenway

Fujioka

et al. 2008

Int J Obes

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Objective: To determine the magnitude and determinants of weight loss in humans exposed to betahistine, a centrally acting histamine-1 (H-1) agonist and partial histamine-3 (H-3) antagonist. Design: A multicenter randomized, placebo-controlled dose-ranging weight loss trial with a 12-week treatment period. Subjects: Two hundred and eighty-one obese but otherwise healthy participants. Measurements: Weight and obesity-related comorbidities at baseline and at the end of the intervention. Results: Betahistine, at the doses tested, did not induce significant weight loss. With the exception of headache, no difference in adverse effect profile was noted between placebo and treatment groups. Subgroup analysis revealed that age below 50 years, ethnicity (non-Hispanics) and gender (women) were the strongest predictors of weight loss in this population. When these three factors were combined together, the betahistine 48 mg group (n ¼ 23) lost À4.24 ± 3.87 kg, whereas the placebo group (n ¼ 25) lost À1.65±2.96 kg during this time period (P ¼ 0.005). Conclusion: Betahistine, at the doses tested, induced significant weight loss with minimal adverse events only in women below 50 years.

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“…Also, an acute injection of histamine into the lateral ventricle of rats has been shown to reduce food intake [14]. In addition, intraperitoneal injection of L -histidine, the histamine precursor, has been shown to have the same effect as histamine, reducing food intake [15,16,17]. This is possibly the result of an increase in brain histamine, after L -histidine has been transported to the brain and converted to histamine by the HDC enzyme.…”

Section: The Histaminergic System and Neuroendocrine Regulation Of Apmentioning

confidence: 99%

Histamine and the Regulation of Body Weight

Jørgensen

Knigge²,

Warberg³

et al. 2007

Neuroendocrinology

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Energy intake and expenditure is regulated by a complex interplay between peripheral and central factors. An exhaustive list of peptides and neurotransmitters taking part in this complex regulation of body weight exists. Among these is histamine, which acts as a central neurotransmitter. In the present article we review current evidence pointing at an important role of histamine in the regulation of appetite and metabolism. Studies using both knockout mouse models as well as pharmacological studies have revealed that histamine acts as an anorexigenic agent via stimulation of histamine H₁ receptors. One effect of histamine in the regulation of appetite is to act as a mediator of the inhibitory effect of leptin on appetite. It seems that histamine may attenuate and delay the development of leptin resistance in high-fat-diet-induced obesity. Furthermore, histamine may also act to accelerate lipolysis. Based on the current evidence of the involvement of histamine in the regulation of body weight, the histaminergic system is an obvious target for the development of pharmacological agents to control obesity. At present, H₃ receptor antagonists that stimulate the histaminergic system may be the most promising histaminergic drugs for antiobesity therapy.

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Antihistaminic drugs increase feeding, while histidine suppresses feeding in rats

Cited by 70 publications

References 19 publications

Antipsychotic drug-induced weight gain mediated by histamine H₁receptor-linked activation of hypothalamic AMP-kinase

Antipsychotic drug-induced weight gain mediated by histamine H₁receptor-linked activation of hypothalamic AMP-kinase

Effect of histaminergic manipulation on weight in obese adults: a randomized placebo controlled trial

Histamine and the Regulation of Body Weight

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Antihistaminic drugs increase feeding, while histidine suppresses feeding in rats

Cited by 70 publications

References 19 publications

Antipsychotic drug-induced weight gain mediated by histamine H1receptor-linked activation of hypothalamic AMP-kinase

Antipsychotic drug-induced weight gain mediated by histamine H1receptor-linked activation of hypothalamic AMP-kinase

Effect of histaminergic manipulation on weight in obese adults: a randomized placebo controlled trial

Histamine and the Regulation of Body Weight

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Product

Resources

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Antipsychotic drug-induced weight gain mediated by histamine H₁receptor-linked activation of hypothalamic AMP-kinase

Antipsychotic drug-induced weight gain mediated by histamine H₁receptor-linked activation of hypothalamic AMP-kinase