Results 171 to 180 of about 10,873 (200)

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, Remko A, Bakker, Rob, Leurs   +2 more
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H3 Receptor Miniseries: Histamine and H3 receptor in alcohol-related behaviors.

The Journal of Pharmacology and Experimental Therapeutics, 2020
Data from rat models for alcohol preference and histidine decarboxylase knockout (HDC KO) mice suggest that brain histamine regulates alcohol-related behaviors. Histamine levels are higher in alcohol-preferring than in alcohol-nonpreferring rat brains, and expression of histamine H(3) receptor (H(3)R) is different in key areas for addictive behavior. H(
Panula Pertti, Nuutinen Saara, Panula Pertti, Nuutinen Saara   +3 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., Morisset, S., Gbahou, Tedohe Florence   +2 more
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Fluorinated non-imidazole histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2009
Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (
K, Isensee, M, Amon, A, Garlapati, A, Galaparti, X, Ligneau, J-C, Camelin, M, Capet, J-C, Schwartz, H, Stark   +8 more
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Histamine H3-receptor isoforms

Inflammation Research, 2004
Increasing evidence supports a role for HA as a neurotransmitter and neuromodulator in various brain functions, including emotion, cognition, and feeding. The recent cloning of the histamine H3 receptor allowed for the subsequent cloning of a variety of H3 receptor isoforms from different species as well as the H4 receptor.
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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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