International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors
Pertti Panula,Paul L. Chazot,Marlon D. Cowart,Ralf Gutzmer,Rob Leurs,Wai L. S. Liu,Holger Stark,Robin L. Thurmond,Helmut L. Haas +8 more
Reads0
Chats0
TLDR
The H3R is an autoreceptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons, a block of these actions promotes waking and the development of anti-inflammatory drugs is anticipated.Abstract:
Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues. Its physiological functions are mediated by four 7-transmembrane G protein–coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. The receptors display molecular heterogeneity and constitutive activity. H1R antagonists are long known antiallergic and sedating drugs, whereas the H2R was identified in the 1970s and led to the development of H2R-antagonists that revolutionized stomach ulcer treatment. The crystal structure of ligand-bound H1R has rendered it possible to design new ligands with novel properties. The H3R is an autoreceptor and heteroreceptor providing negative feedback on histaminergic and inhibition on other neurons. A block of these actions promotes waking. The H4R occurs on immuncompetent cells and the development of anti-inflammatory drugs is anticipated.read more
Citations
More filters
The physiological action of β-iminazolylethylamine
H. H. Dale,P. P. Laidlaw +1 more
TL;DR: Ackermann and Kutscher as mentioned in this paper showed that the ergot base, though closely related to 8-iminazolylethylamine, is not identical with it.
Journal ArticleDOI
Monoaminergic neuropathology in Alzheimer's disease.
Goran Šimić,Mirjana Babić Leko,Selina Wray,Charles R. Harrington,Ivana Delalle,Nataša Jovanov-Milošević,Danira Bažadona,Luc Buée,Rohan de Silva,Giuseppe Di Giovanni,Claude M. Wischik,Patrick R. Hof +11 more
TL;DR: Special emphasis is given to the serotonergic dorsal raphe nucleus (DRN) and noradrenergic LC, among the first to be affected by tau protein abnormalities in the course of sporadic AD, causing behavioral and cognitive symptoms of variable severity.
Journal ArticleDOI
The Histamine H3 Receptor: Structure, Pharmacology, and Function.
Gustavo Nieto-Alamilla,Ricardo Márquez-Gómez,Ana-Maricela García-Gálvez,Guadalupe-Elide Morales-Figueroa,José-Antonio Arias-Montaño +4 more
TL;DR: The characteristics of the H3R are reviewed, namely, its structure, constitutive activity, isoforms, signal transduction pathways, regional differences in expression and localization, selective agonist, antagonists and inverse agonists, dimerization with other neurotransmitter receptors, and the main presynaptic and postsynaptic effects resulting from its activation.
Journal ArticleDOI
Multi-target design strategies for the improved treatment of Alzheimer's disease
TL;DR: Nine major targets associated with AD are highlighted and eleven multi-target design strategies classified by the involvement of AChE and related promising compounds for improved therapy of AD in recent years are described based on the nine major targets.
References
More filters
Journal ArticleDOI
Unidentified curved bacilli in the stomach of patients with gastritis and peptic ulceration
Barry J. Marshall,J R Warren +1 more
TL;DR: The bacteria were present in almost all patients with active chronic gastritis, duodenal ulcer, or gastric ulcer and thus may be an important factor in the aetiology of these diseases.
Journal ArticleDOI
Definition and antagonism of histamine H 2 -receptors.
TL;DR: H2-receptor antagonist, a new group of drugs, may help to unravel the physiology of histamine and gastrin.
Journal ArticleDOI
Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor.
TL;DR: It is shown here that histamine inhibits its own release from depolarized slices of rat cerebral cortex, an action apparently mediated by a class of receptor (H3) pharmacologically distinct from those previously characterized, that is, the H1 and H2 receptors.
Journal ArticleDOI
Cloning and characterization of chi-1: a developmentally regulated member of a novel class of the ionotropic glutamate receptor family
TL;DR: A cloned member of a novel class of the rat ionotropic glutamate receptor family, termed chi-1, exhibits an average identity to NMDA subunits and 23% to non-NMDA sub units, which suggests that chi- 1 may specifically interact with NMDA receptor subunits.
Journal ArticleDOI
Structural diversity of G protein-coupled receptors and significance for drug discovery
TL;DR: This article aims to provide a comprehensive overview of the five main human GPCR families with a focus on gene repertoire, general ligand preference, common and unique structural features, and the potential for future drug discovery.