Identification of rat H3 receptor isoforms with different brain expression and signaling properties.

@article{Drutel2001IdentificationOR,
  title={Identification of rat H3 receptor isoforms with different brain expression and signaling properties.},
  author={G. Drutel and N. Peitsaro and K. Karlstedt and K. Wieland and M. Smit and H. Timmerman and P. Panula and R. Leurs},
  journal={Molecular pharmacology},
  year={2001},
  volume={59 1},
  pages={
          1-8
        }
}
We identified the cDNAs of three functional rat H3 receptor isoforms (H3A, H3B, and H3C) and one nonfunctional truncated H3 receptor (H3T). The H3A, H3B, and H3C receptor isoforms vary in the length of their third intracellular loop; the H3B and H3C receptor lack 32 and 48 amino acids, respectively. Transient expression of the H3A, H3B, and H3C receptors in COS-7 cells results in high affinity binding for the H3 antagonist [125I]iodophenpropit, which is displaced by selective H3 agonists and… Expand
[Identification and characterization of histamine H4 receptor].
  • T. Oda, S. Matsumoto
  • Chemistry, Medicine
  • Nihon yakurigaku zasshi. Folia pharmacologica Japonica
  • 2001
TLDR
The discovery of this receptor subtype will unveil a new phase for determining the physiological role of histamine, and there needs much additional work on characterization of the H4 receptor. Expand
Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms
TLDR
In situ hybridization histochemistry showed that the distribution of H3‐receptor mRNAs in the mouse brain is rather similar to that previously reported in the rat brain, however, the autoradiographic and cellular expression patterns observed in several brain areas such as the thalamus or hippocampus reveal important differences between the two species. Expand
The Histamine H3 Receptor: Structure, Pharmacology, and Function
TLDR
The characteristics of the H3R are reviewed, namely, its structure, constitutive activity, isoforms, signal transduction pathways, regional differences in expression and localization, selective agonist, antagonists and inverse agonists, dimerization with other neurotransmitter receptors, and the main presynaptic and postsynaptic effects resulting from its activation. Expand
Constitutive activity of the recombinant and native histamine H3 receptor
TLDR
Constitutive activity of presynaptic H3 autoreceptors modulates histamine release from cortical synaptosomes in vitro and controls histamine neuron activity in vivo, implying that inverse agonists rather than neutral antagonists may find therapeutic applications. Expand
Structure and expression of the human histamine H4-receptor gene.
TLDR
The characterization by genomics-based approach of the human H4-receptor gene structure will facilitate the elucidation of its transcriptional control by factors secreted during inflammatory responses. Expand
Identification and Characterization of ZEL-H16 as a Novel Agonist of the Histamine H3 Receptor
TLDR
It is demonstrated that treatment of ZEL-H16 resulted in intensive H3 receptor internalization and delayed recycling to the cell surface as compared to that of control with treatment of histamine, which might serve as a pharmacological tool for future investigations or as possible therapeutic agent of H3R. Expand
[Isoforms of the human histamine H3 receptor: Generation, expression in the central nervous system and functional implications].
TLDR
The evidence for the generation of human H3R isoforms, their expression, and the available information regarding the functionality of such receptors are reviewed. Expand
Discovery of Naturally Occurring Splice Variants of the Rat Histamine H3 Receptor That Act as Dominant-Negative Isoforms
TLDR
It is shown that in rat brain, the H3R mRNA expression levels are modulated upon treatment with the convulsant pentylenetetrazole, suggesting that the rH3R isoforms described herein represent a novel physiological mechanism for controlling the activity of the histaminergic system. Expand
Molecular cloning and pharmacology of functionally distinct isoforms of the human histamine H3 receptor
TLDR
Multiple, functionally distinct, alternatively spliced isoforms of the human H(3) receptor are described, suggesting at least six distinct receptor isoforms, of which isoforms 1, 2, and 4, encode functional proteins. Expand
Generation and characterisation of the first anti-human H3R445/453 isoform specific antibody probe
TLDR
Information is provided on a new anti-human H3R445/453 receptor isoform specific antibody that aims to define the importance of human H3 receptor heterogeneity, and the signalling and functional properties of the isoforms need to be characterised. Expand
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