Abstract
Obesity is the effect of imbalance between energy intake and expenditure and forms a fundamental basis of the metabolic syndrome. A number of substances implicated in the regulation of energy metabolism represent opportunities for anti-obesity drug development. Neuronal histamine and its receptors have been shown to regulate energy metabolism and are considered as anti-obesity targets. Several histamine receptor subtypes have been identified; of these, histamine H1 and H3 receptors (H1-R and H3-R) have been specifically recognized as mediators of energy intake and expenditure. In addition, several histamine drugs related to H1-R and H3-R, have been shown to attenuate body weight gain both in rodent and human. These results provide the reagents for histamine receptors biology and may find applications in the treatment of obesity and related metabolic disorders. In this review, the development of agonists and antagonists of histamine receptors are provided.
Keywords: Histamine, food intake, obesity, histamine H1 receptors, histamine H3 receptors, histidine decarboxylase, brain, metabolic syndrome, histamine H1, H3 receptors, hypertension, diabetes, stroke, N-methyltransferase, hippocampus, amygdala, basal ganglia, betahistine, chlorpheniramine, antiobesity agent, neurotransmitter, Thioperamide, R-methylhistamine, anorectic effects, anti-psychotic olanzapine caused, hyperphagia, hypothalamic AMP-kinase, arcuate nu-cleus, ventromedial nucleus
Current Medicinal Chemistry
Title: Neuronal Histamine and its Receptors: Implication of the Pharmacological Treatment of Obesity
Volume: 17 Issue: 36
Author(s): T. Masaki and H. Yoshimatsu
Affiliation:
Keywords: Histamine, food intake, obesity, histamine H1 receptors, histamine H3 receptors, histidine decarboxylase, brain, metabolic syndrome, histamine H1, H3 receptors, hypertension, diabetes, stroke, N-methyltransferase, hippocampus, amygdala, basal ganglia, betahistine, chlorpheniramine, antiobesity agent, neurotransmitter, Thioperamide, R-methylhistamine, anorectic effects, anti-psychotic olanzapine caused, hyperphagia, hypothalamic AMP-kinase, arcuate nu-cleus, ventromedial nucleus
Abstract: Obesity is the effect of imbalance between energy intake and expenditure and forms a fundamental basis of the metabolic syndrome. A number of substances implicated in the regulation of energy metabolism represent opportunities for anti-obesity drug development. Neuronal histamine and its receptors have been shown to regulate energy metabolism and are considered as anti-obesity targets. Several histamine receptor subtypes have been identified; of these, histamine H1 and H3 receptors (H1-R and H3-R) have been specifically recognized as mediators of energy intake and expenditure. In addition, several histamine drugs related to H1-R and H3-R, have been shown to attenuate body weight gain both in rodent and human. These results provide the reagents for histamine receptors biology and may find applications in the treatment of obesity and related metabolic disorders. In this review, the development of agonists and antagonists of histamine receptors are provided.
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Cite this article as:
Masaki T. and Yoshimatsu H., Neuronal Histamine and its Receptors: Implication of the Pharmacological Treatment of Obesity, Current Medicinal Chemistry 2010; 17 (36) . https://dx.doi.org/10.2174/092986710794182944
DOI https://dx.doi.org/10.2174/092986710794182944 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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