Agonist potency at some neurotransmitter receptors has been shown to be regulated by
voltage, a mechanism which has been suggested to play a crucial role in the regulation of …

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 …

The histamine H3 receptor mediates inhibitory responses in the nervous system. Here, we
demonstrate the coupling of the human histamine H3 receptor to G protein-coupled inward …

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 …

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 …

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 …

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 …

Abstract Histamine H 3 receptors (H 3 Rs) modulate the function of the nervous system at the
pre-and post-synaptic levels. In this work we aimed to determine whether, as other G protein …

Abstract Histamine H 3 receptors (H 3 Rs) signal through Gα i/o proteins and are found in
neuronal cells as auto-and hetero-receptors. Alternative splicing of the human H 3 R (hH 3 …

To examine the role of the C terminal tail in H2 receptor regulation, three cDNAs, encoding
truncated histamine H2 receptor mutants (H2T295, H2T307, and H2T341), were constructed …