Results 231 to 240 of about 41,179 (270)
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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
openaire   +3 more sources

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.
Anayansi Molina-Hernández   +3 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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The Histamine H3 Receptor

2000
Histamine is widely distributed in the body, although with marked quantitative differences in the various species and tissues, and it produces a variety of biological effects by interacting with specific receptors on the surface of target cells.
CORUZZI G.   +3 more
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Histamine H3 receptor ligands by hybrid virtual screening, docking, molecular dynamics simulations, and investigation of their biological effects

Chemical Biology and Drug Design, 2019
Histamine H3 receptors (H3R), belonging to G‐protein coupled receptors (GPCR) class A superfamily, are responsible for modulating the release of histamine as well as of other neurotransmitters by a negative feedback mechanism mainly in the central ...
N. Ghamari   +5 more
semanticscholar   +1 more source

6 The Histamine H3 Receptor and its Ligands

2001
Publisher Summary This chapter explores that the detection of the histamine H3 receptor was first performed with burimamide, an H2/H3-receptor antagonist formerly used for the first differentiation between histamine H1 and H2 receptors. The existence of H3 receptors is proven with selective agonists and antagonists using classical pharmacological ...
Walter Schunack   +6 more
openaire   +3 more sources

Histamine and H3 Receptor in Alcohol-Related Behaviors

The Journal of Pharmacology and Experimental Therapeutics, 2011
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(
Saara Nuutinen, Pertti Panula
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An update on histamine H3 receptors and gastrointestinal functions

Digestive Diseases and Sciences, 1995
The distribution and functions of histamine H3 receptors in the gastrointestinal tract is reviewed with particular reference to the effects on gastric acid secretion, mucosal protection, and intestinal motility. Histamine H3 receptor activation has negative effects on acid secretion induced by indirect secretagogues in cats, dogs, and rabbits; less ...
Giulio Bertaccini, Gabriella Coruzzi
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Synthesis of radioligands for the histamine H3 receptor

1998
Publisher Summary This chapter discusses the synthesis of radioligands for the histamine H 3 receptor. Radiolabelled receptor ligands are of great importance for studying receptor–ligand interactions. Pharmacologists use radiolabelled compounds, not only for in-depth pharmacological research—for example, distribution—but also for screening compounds,
Windhorst, Albert D.   +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
openaire   +2 more sources

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