Results 211 to 220 of about 13,967 (254)

Non-imidazole heterocyclic histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2003
Continued exploration of the SAR around the lead imidazopyridine histamine H(3) antagonist 1 has led to the discovery of several related series of heterocyclic histamine H(3) antagonists. The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described.
Wenying, Chai, J Guy, Breitenbucher, Annette, Kwok, Xiaobing, Li, Victoria, Wong, Nicholas I, Carruthers, Timothy W, Lovenberg, Curt, Mazur, Sandy J, Wilson, Frank U, Axe, Todd K, Jones   +10 more
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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, Olga A, Sergeeva, Helmut L, Haas   +2 more
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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, Héctor, Flores-Herrera, Guadalupe, García-López, Anayansi, Molina-Hernández   +3 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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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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Phencyclidine blocks histamine H3-receptors in rat brain

European Journal of Pharmacology, 1988
Phencyclidine (PCP) was examined for its ability to modulate histamine release from rat brain slices labeled with L-[3H]histidine. PCP failed to mimic but completely reversed the autoinhibitory effect of histamine at H3-receptors with an apparent Ki value of 13 +/- 3 microM.
J M, Arrang, N, Defontaine, J C, Schwartz   +2 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, G, Coruzzi, M, Adami, C, Pozzoli, E, Gambarelli   +4 more
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Design of histamine H3-receptor agonists and antagonists

European 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
W, Schunack, H, Stark
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Rasagiline derivatives combined with histamine H3 receptor properties

Bioorganic & Medicinal Chemistry Letters, 2019
The irreversible monoamine oxidase B (MAO B) inhibitor rasagiline has been described with multiple disease modifying effects in vitro on models of Parkinson's disease. The combination of this established drug to recently developed histamine H3 receptor (H3R) antagonist elements gives new impetus to the design of multitargeting ligands.
K, Lutsenko, S, Hagenow, A, Affini, D, Reiner, H, Stark   +4 more
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