International union of basic and clinical pharmacology. XCVIII. Histamine receptors

P Panula, PL Chazot, M Cowart, R Gutzmer… - Pharmacological …, 2015 - ASPET
Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues.
Its physiological functions are mediated by four 7-transmembrane G protein–coupled …

The histaminergic network in the brain: basic organization and role in disease

P Panula, S Nuutinen - Nature Reviews Neuroscience, 2013 - nature.com
Histamine acts as a modulatory neurotransmitter in the mammalian brain. It has an important
role in the maintenance of wakefulness, and dysfunction in the histaminergic system has …

Sleep neurobiology from a clinical perspective

RA España, TE Scammell - Sleep, 2011 - academic.oup.com
Many neurochemical systems interact to generate wakefulness and sleep. Wakefulness is
promoted by neurons in the pons, midbrain, and posterior hypothalamus that produce …

The histamine H3 receptor: from discovery to clinical trials with pitolisant

JC Schwartz - British journal of pharmacology, 2011 - Wiley Online Library
The third histamine receptor was discovered in 1983 by a traditional pharmacological
approach, consisting of assessing the inhibitory effect of histamine on its own release from …

The histamine H3 receptor: an attractive target for the treatment of cognitive disorders

TA Esbenshade, KE Browman… - British journal of …, 2008 - Wiley Online Library
The histamine H3 receptor, first described in 1983 as a histamine autoreceptor and later
shown to also function as a heteroreceptor that regulates the release of other …

Histamine receptors in the CNS as targets for therapeutic intervention

MB Passani, P Blandina - Trends in pharmacological sciences, 2011 - cell.com
Histamine has long been known to trigger allergic reactions and gastric acid secretion.
However, it was later discovered that, in the brain, histamine regulates basic homeostatic …

An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: studies in orexin−/− mice and patients

JS Lin, Y Dauvilliers, I Arnulf, H Bastuji, C Anaclet… - Neurobiology of …, 2008 - Elsevier
Narcolepsy is characterized by excessive daytime sleepiness (EDS), cataplexy, direct
onsets of rapid eye movement (REM) sleep from wakefulness (DREMs) and deficiency of …

Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease

JD Brioni, TA Esbenshade, TR Garrison… - … of Pharmacology and …, 2011 - ASPET
H3 antagonists increase the release of brain histamine, acetylcholine, noradrenaline, and
dopamine, neurotransmitters that are known to modulate cognitive processes. The ability to …

Zebrafish: An in vivo model for the study of neurological diseases

JD Best, WK Alderton - Neuropsychiatric disease and treatment, 2008 - Taylor & Francis
As the population ages, there is a growing need for effective therapies for the treatment of
neurological diseases. A limited number of therapeutics are currently available to improve …

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases

D Vanda, P Zajdel, M Soural - European Journal of Medicinal Chemistry, 2019 - Elsevier
This article provides an overview of compounds based on imidazo [1, 2-a] pyridine, imidazo
[1, 5-a] pyridine, imidazo [4, 5-b] pyridine and imidazo [4, 5-c] pyridine scaffolds, which act as …