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Histamine H3 Receptor Agonists
Mini-Reviews in Medicinal Chemistry, 2004The 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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Molecular aspects of the histamine H3 receptor
Biochemical Pharmacology, 2007The 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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H3 Receptor Miniseries: Histamine and H3 receptor in alcohol-related behaviors.
The Journal of Pharmacology and Experimental Therapeutics, 2020Data 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 +3 more
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Constitutive activity of the histamine H3 receptor
Trends in Pharmacological Sciences, 2007Constitutive 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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Fluorinated non-imidazole histamine H3 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2009Fluorine 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 +8 more
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Histamine H3-receptor isoforms
Inflammation Research, 2004Increasing 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, 2003Continued 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 +10 more
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Histamine H3 Receptors and Sleep-Wake Regulation
The Journal of Pharmacology and Experimental Therapeutics, 2011The 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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