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Histamine H3 Receptors and Sleep-Wake Regulation

The Journal of Pharmacology and Experimental Therapeutics, 2011
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 ...
Jian-Sheng, Lin   +2 more
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Molecular aspects of the histamine H3 receptor

Biochemical Pharmacology, 2007
The cloning of the histamine H(3) receptor (H(3)R) cDNA in 1999 by Lovenberg et al. [10] allowed detailed studies of its molecular aspects and indicated that the H(3)R can activate several signal transduction pathways including G(i/o)-dependent inhibition of adenylyl cyclase, activation of phospholipase A(2), Akt and the mitogen activated kinase as ...
Gerold, Bongers   +2 more
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Constitutive activity of the histamine H3 receptor

Trends in Pharmacological Sciences, 2007
Constitutive activity has been mainly recorded for numerous overexpressed and/or mutated receptors. The histamine H(3) receptor (H(3)R) is a target of choice to study the physiological relevance of this process. In rodent brain, postsynaptic H(3)Rs show high constitutive activity, and presynaptic H(3) autoreceptors that show constitutive activity have ...
Arrang, J.M.   +2 more
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The other side of the histamine H3 receptor

Trends in Neurosciences, 2014
Although histamine H3 receptors are predominantly known as presynaptic receptors, regulating the release of neurotransmitters such as dopamine, acetylcholine, and histamine, in the striatal complex the vast majority of these receptors are actually located on the other side, in other words postsynaptically.
Bart A, Ellenbroek, Bibinaz, Ghiabi
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Imaging Histamine H3 Receptors with Positron Emission Tomography

2021
Positron emission tomography (PET) provides a unique tool to study the biochemistry of the human brain in vivo. By using PET probes that are binding selectively to certain receptor subtypes, brain PET allows the quantification of receptor levels in various brain areas of human subjects.
Pablo Martín, Rusjan, Bernard, Le Foll
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Central Histamine, the H3-Receptor and Obesity Therapy

CNS & Neurological Disorders - Drug Targets, 2019
The brain histaminergic system plays a pivotal role in energy homeostasis, through H1- receptor activation, it increases the hypothalamic release of histamine that decreases food intake and reduces body weight. One way to increase the release of hypothalamic histamine is through the use of antagonist/inverse agonist for the H3-receptor.
Néstor F, Díaz   +3 more
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Structure–activity relationships of arylbenzofuran H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2005
An SAR study of histamine H3 receptor antagonists based on substituted (R)-2-methyl-1-[2-(5-phenyl-benzofuran-2-yl)-ethyl]-pyrrolidines is presented.
Gregory A, Gfesser   +6 more
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Histamine H3 receptors: an overview.

The Italian journal of gastroenterology, 1992
Histamine H3 receptors represent a new class of prejunctional receptors, which, first described as modulators of histamine synthesis and release in the central nervous system, were subsequently found to occur also in peripheral tissues. They may behave both as autoreceptors located in histaminergic neurons and as heteroreceptors localized in adrenergic,
G, Bertaccini   +4 more
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Histamine H3 Receptor Function and Ligands: Recent Developments

Mini-Reviews in Medicinal Chemistry, 2012
Histamine H3 receptors are found mostly in central nervous system involved in the regulation of release of various neurotransmitters in brain. They have been implicated in diverse potential therapeutic applications such as sleep-wake disorders, attention-deficient hyperactivity disorder, epilepsy, cognitive impairment and obesity.
Mahaveer, Singh, Hemant R, Jadhav
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H3 Receptor Miniseries: The histamine H3 receptor and eating behavior

2011
Interest in the histaminergic system as a potential target for the treatment of feeding disorders is driven by the unsatisfactory history of the pharmacotherapy of obesity. Eating behavior is regulated by a complex interplay of central neurotransmitter systems, peripheral endocrine stimuli, the circadian rhythm, and environmental cues, all factors that
PASSANI, MARIA BEATRICE   +2 more
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