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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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Role of the Histamine H3 Receptor in the Central Nervous System

Handbook of Experimental Pharmacology, 2016
The Gi/o protein-coupled histamine H3 receptor is distributed throughout the central nervous system including areas like cerebral cortex, hippocampus and striatum with the density being highest in the posterior hypothalamus, i.e. the area in which the histaminergic cell bodies are located.
M. Kathmann, Eberhard Schlicker
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Histamine H3 Receptor Agonists

Mini-Reviews in Medicinal Chemistry, 2004
The SAR of H3 ligands has been difficult to evaluate because of species differences, multiple isoforms and constitutive activity, among other complicating factors. A review is given of the sometimes-conflicting affinity, activity and efficacy data of H3 agonists that has been described in literature to date.
I J P De Esch, K J Belzar
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Dual-targeting approach on histamine H3 and sigma-1 receptor ligands as promising pharmacological tools in the treatment of CNS-linked disorders.

Current Medicinal Chemistry, 2020
With the recent market approval of Pitolisant (Wakix®), the interest in clinical application for novel multifunctional histamine H3 receptor antagonists has clearly increased.
K. Szczepańska   +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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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 ...
Rob Leurs   +2 more
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Design of histamine H3-receptor agonists and antagonists [PDF]

open access: possibleEuropean Journal of Drug Metabolism and Pharmacokinetics, 1994
The development of highly potent and selective ligands for the characterization of histamine H3-receptors is reviewed. In the field of agonists stereoselectively methylated derivatives of the natural ligand are found to have the desired pharmacodynamic properties. Pharmacokinetic properties could be improved by forming bioreversible azomethine prodrugs
Walter Schunack, Holger Stark
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