Ligand pharmacology of histamine H3-receptors is species-dependent. In previous studies,
two amino acids in transmembrane domain 3 (TM III) were shown to play a significant role. In …

Starting from the sequence of the human histamine H3 receptor (hH3R) cDNA, we have
cloned the corresponding rat cDNA. Whereas the two deduced proteins show 93.5% overall …

Various histamine derivatives were investigated at the human H3 receptor (H3R) and H4
receptor (H4R) stably expressed in human embryonic kidney (HEK)‐293 cells using [125I] …

Species isoforms of histamine H2-, H3-, and H4-receptors differ in their pharmacological
properties. The study aim was to dissect differences between the human H1R (hH1R) and …

The recently identified histamine H 4 receptor has revealed a potential new complexity for
the role of histamine in the immune system. To begin to understand the role of this receptor …

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 …

The histamine H4 receptor (H4R) is involved in the chemotaxis of leukocytes and mast cells
to sites of inflammation and is suggested to be a potential drug target for asthma and allergy …

Constitutive activation of G-protein-coupled receptors is a well recognized phenomenon,
and G-protein-coupled receptor antagonists have been found to possess inverse agonist …

The human histamine H4-receptor (hH4R) possesses high constitutive activity and, like the
human H1-receptor (hH1R), is involved in the pathogenesis of type-I allergic reactions. The …

Background and Purpose Some histamine H 4 receptor ligands act as inverse agonists at
the human H4 receptor (hH4R), a receptor with exceptionally high constitutive activity, but as …