Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues.
Its physiological functions are mediated by four 7-transmembrane G protein–coupled …

Among the four G protein–coupled receptors (H1–H4) identified as mediators of the biologic
effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive …

The histaminergic system is exclusively localized within the posterior hypothalamus with
projection to almost all the major regions of the central nervous system. Strong and …

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 …

BACKGROUND: Histamine is a potent mediator of itch in humans, yet histamine H1 receptor
antagonists have been shown to be of limited use in the treatment of certain chronic pruritic …

6-[(3-Cyclobutyl-2, 3, 4, 5-tetrahydro-1 H-3-benzazepin-7-yl) oxy]-N-methyl-3-
pyridinecarboxamide hydrochloride (GSK189254) is a novel histamine H3 receptor …

H3 antagonists increase the release of brain histamine, acetylcholine, noradrenaline, and
dopamine, neurotransmitters that are known to modulate cognitive processes. The ability to …

The neurotransmitter histamine receives less attention compared with other biogenic
amines, because of its moderate action in the central nervous system (CNS). However …

The histamine H3 receptor plays a regulatory role in the pre-synaptic release of histamine
and other neurotransmitters, making it an attractive target for CNS indications including …

Within the recent years novel lead optimisations for histamine H3 receptor antagonists made
their way from bench to bedside. Structure–activity relationships, cross-affinities and side …