Activity-restoring mutations in the histamine H<sub>3</sub> receptor increase constitutive activity and reduce structural stability. [PDF]
Abstract The histamine H3 receptor (H3R) is a class A G protein‐coupled receptor (GPCR) that regulates neurotransmitter release in the central nervous system. Although structures of H3R in both inactive and active states have been elucidated, the functional roles of specific residues remain unclear.
Nakajima A +6 more
europepmc +2 more sources
Letter to the Editor in Response to "Efficacy and Safety of Histamine H3 Receptor Antagonist/Inverse Agonist Including Betahistine for Schizophrenia: A Systematic Review and Meta-Analysis" by Nishii et al. [PDF]
Neuropsychopharmacology Reports, Volume 45, Issue 4, December 2025.
Farhan M.
europepmc +2 more sources
Pitolisant Inhibits Alcohol Drinking and Improves Withdrawal Negative Affect Through Lateral Habenula Histaminergic Signaling in Mice. [PDF]
Pitolisant, an FDA‐approved H3R antagonist, counteracts the rewarding and sedative effects of ethanol, reduces alcohol intake, and alleviates the negative affect during withdrawal. This might occur via the antagonism of presynaptic autoreceptors and heteroreceptors H3Rs in the lateral habenula, thereby activating the H2R/p‐CREB/BDNF signaling and ...
Zhao Y +13 more
europepmc +2 more sources
The role of the host—Neutrophil biology
Abstract Neutrophilic polymorphonuclear leukocytes (neutrophils) are myeloid cells packed with lysosomal granules (hence also called granulocytes) that contain a formidable antimicrobial arsenal. They are terminally differentiated cells that play a critical role in acute and chronic inflammation, as well as in the resolution of inflammation and wound ...
Iain L. C. Chapple +4 more
wiley +1 more source
Neurotransmitters and Immunity: Molecular Mechanisms, Biological Functions, Diseases, and Potential Therapeutic Targets. [PDF]
Role of neurotransmitters in multiple pathological processes. Various neurotransmitters, including ACh, EPI, NE, 5‐HT, histamine, DA, glutamate, GABA, and neuropeptides participate in regulating key pathological events, including tumor proliferation, tumor migration, remodeling of the immune microenvironment, and the development of NDDs and ...
Li G +13 more
europepmc +2 more sources
Antihistaminergics and inverse agonism. Potential therapeutic applications [PDF]
The accurate characterization of the molecular mechanisms involved in the action of receptor ligands is important for their appropriate therapeutic use and safety.
Davio, Carlos Alberto +4 more
core +13 more sources
Assessment of [125I]WYE-230949 as a novel histamine H3 receptor radiopharmaceutical. [PDF]
Histamine H3 receptor therapeutics have been proposed for several diseases such as schizophrenia, attention deficit hyperactivity disorder, Alzheimer's disease and obesity.
David Y Lewis +4 more
doaj +1 more source
Histamine and migraine revisited: mechanisms and possible drug targets
Objective To review the existing literature on histamine and migraine with a focus on the molecule, its receptors, its use in inducing migraine, and antihistamines in the treatment of migraine. Background Histamine has been known to cause a vascular type
Jacob Worm +2 more
doaj +1 more source
H3 histamine receptor-mediated activation of protein kinase calpha inhibits the growth of cholangiocarcinoma in vitro and in vivo [PDF]
Histamine regulates functions via four receptors (HRH1, HRH2, HRH3, and HRH4). The D-myo-inositol 1,4,5-trisphosphate (IP(3))/Ca(2+)/protein kinase C (PKC)/mitogen-activated protein kinase pathway regulates cholangiocarcinoma growth.
A. Vetuschi +13 more
core +1 more source
Calyx and dimorphic neurons of mouse Scarpa's ganglion express histamine H3 receptors
Background Histamine-related drugs are commonly used in the treatment of vertigo and related vestibular disorders. The site of action of these drugs however has not been elucidated yet.
Zucca Gianpiero +5 more
doaj +1 more source

