We combined in a previously derived three-dimensional model of the histamine H 1 receptor
(Ter Laak, AM, Timmerman, H., Leurs, H., Nederkoorn, PHJ, Smit, MJ, and Donne-Op den …

Monovalent ions differently affect ligand binding to G protein-coupled receptors (GPCRs) by
as yet poorly defined mechanisms. In particular, NaCl often decreases the affinity of agonists …

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 …

Agonist-independent activity of G-protein-coupled receptor, also referred to as constitutive
activity, is a well-documented phenomenon and has been reported recently for both the …

We have recently identified three splice isoforms of the histamine H3 receptor in multiple
brain regions of cynomolgus monkey (Macaca fascicularis). Two of the novel isoforms …

Previously, we have shown that asparagine207 in the fifth transmembrane domain of the
histamine H1 receptor is crucial for the binding of the Nτ-nitrogen of the imidazole ring of …

We have used alanine scanning mutagenesis to identify residues in transmembrane domain
5 of the histamine H3 receptor that are important for agonist binding. All of the mutants …

The present study focused on the desensitization process of the H2 receptor in U937 cells
and the recovery of the cyclic AMP (cAMP) response. Treatment of U937 leukemic cells with …

In this study we investigated the role of the threonine 203 and the asparagine 207 residues
in the fifth transmembrane domain of the guinea-pig histamine H 1-receptor by site-directed …

Different histamine H3-receptor antagonists have been tested in displacement studies at
human and rat H3 receptors in stably transfected cells. Based on an actual rhodopsin …