Two Distinct Pathways for Histamine H2 Receptor Down-regulation: H2 LEU124→ ALA RECEPTOR MUTANT PROVIDES EVIDENCE FOR A cAMP-INDEPENDENT …

MJ Smit, E Roovers, H Timmerman… - Journal of Biological …, 1996 - ASBMB
Pretreatment of Chinese hamster ovary cells expressing the histamine H 2 receptor (CHOrH
2 cells) with histamine resulted in a time-dependent (t 1/2≈ 7 h) and dose-dependent (EC …

High Constitutive Activity and a G-Protein-Independent High-Affinity State of the Human Histamine H4-Receptor

EH Schneider, D Schnell, D Papa, R Seifert - Biochemistry, 2009 - ACS Publications
The human histamine H4-receptor (hH4R) is expressed in mast cells and eosinophils and
mediates histamine (HA)-induced chemotaxis via Gi-proteins. For a detailed investigation of …

The histamine H3 receptor: a general presynaptic histaminergic regulatory system?

JF van der Werf, H Timmerman - Trends in Pharmacological Sciences, 1989 - cell.com
The histamine H3 receptor was first postulated as a novel class of histamine receptor by the
research group of JC Schwartz'in 1983. Using rat brain tissue, this group went on to define a …

Molecular basis for the selective interaction of synthetic agonists with the human histamine H1-receptor compared with the guinea pig H1-receptor

A Straßer, HJ Wittmann, M Kunze, S Elz, R Seifert - Molecular pharmacology, 2009 - ASPET
Previous studies revealed that phenylhistamines and histaprodifens possess higher potency
and affinity at guinea pig histamine H1-receptor (gpH1R) than at human histamine H1 …

The histamine H3 receptor: structure, pharmacology, and function

G Nieto-Alamilla, R Márquez-Gómez… - Molecular …, 2016 - ASPET
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 …

Visualization of agonist-induced internalization of histamine H2 receptors

MJ Smit, H Timmerman, AE Alewijnse, M Punin… - Biochemical and …, 1995 - Elsevier
Histamine H2 receptors were tagged at the N-terminus with the eight amino acid Flag
epitope to allow the immunological identification of the receptor peptide with the monoclonal …

Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases

C Shayo, N Fernandez, BL Legnazzi, F Monczor… - Molecular …, 2001 - ASPET
The histamine H2 receptor (H2r) belongs to the heptahelical receptor family; upon agonist
binding, members of this family activate a G protein and the downstream effector adenylyl …

Histamine H3 receptor binding sites in rat brain membranes: modulations by guanine nucleotides and divalent cations

JM Arrang, J Roy, JL Morgat, W Schunack… - European Journal of …, 1990 - Elsevier
Abstract The binding of [3 H](R) α-methylhistamine, a potent and specific agonist at
histamine H 3 receptors, was investigated with membranes of rat cerebral cortex. In …

Molecular modeling and site-specific mutagenesis of the histamine-binding site of the histamine H4 receptor

N Shin, E Coates, NJ Murgolo, KL Morse, M Bayne… - Molecular …, 2002 - ASPET
The histamine H4 receptor is a novel G-protein–coupled receptor with a unique
pharmacological profile. The distribution of H4 mRNA suggests that it may play a role in the …

The hydrophobic amino acids in putative helix 8 in carboxy-terminus of histamine H3 receptor are involved in receptor-G-protein coupling

A Kuramasu, J Sukegawa, T Sato, E Sakurai… - Cellular signalling, 2011 - Elsevier
Functional roles of putative helix 8 in the carboxy-terminal tail of the human histamine H3
receptor were investigated using deleted and alanine-substituted mutant receptors. While …