| Title |
Characterization of histamine H3 receptors in mouse brain using the H3 antagonist [125I]iodophenpropit
|
|---|---|
| Published in |
Naunyn-Schmiedeberg's Archives of Pharmacology, July 2000
|
| DOI | 10.1007/s002100000227 |
| Pubmed ID | |
| Authors |
Frank P. Jansen, Takatoshi Mochizuki, Kazutaka Maeyama, Rob Leurs, Hendrik Timmerman |
| Abstract |
We have characterized the binding of the histamine H3 receptor antagonist [125I]iodophenpropit to mouse brain. [125I]Iodophenpropit saturably bound to mouse brain membranes with a pKd-value of 9.31+/-0.04 nM and a receptor binding density of 290+/-8 fmol per mg protein. Saturation binding analysis revealed binding of [125I]iodophenpropit to a single class of sites, showing linear Scatchard plots and Hill coefficients not different from unity (nH=0.98+/-0.02). At a concentration of 0.25 nM [125I]iodophenpropit, specific binding represented about 75% of the total binding. Competition binding curves for H3 receptor antagonists were fitted best to a one-site model, showing pKi-values in general accordance with the pA2-values obtained in mouse cerebral cortex. Displacement of [125I]iodophenpropit by the H3 receptor agonists (R)-alpha-methylhistamine, immepip, imetit and histamine were fitted best to a two-site model. Competition binding curves of (R)-alpha-methylhistamine showed a rightward shift upon incubation with GTPgammaS (10 microM), indicating the involvement of G-proteins in H3 agonist binding. In contrast, competition binding curves of the antagonists iodophenpropit, thioperamide and burimamide were not affected by GTPgammaS (10 microM). Autoradiographic experiments showed that [125I]iodophenpropit binding sites were heterogeneously distributed, similarly to the distribution of histamine H3 receptors reported in rat brain. Highest densities were observed in the cerebral cortex, the striatum, the nucleus accumbens, the globus pallidus and the substantia nigra. In conclusion, we have demonstrated that in mouse brain, [125I]iodophenpropit selectively binds to histamine H3 receptors. We also observed that the mouse brain H3 receptors labelled by [125I]iodophenpropit displayed binding characteristics and a distribution similar to rat brain. |
Mendeley readers
The data shown below were compiled from readership statistics for 12 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 12 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Professor | 4 | 33% |
| Student > Ph. D. Student | 3 | 25% |
| Researcher | 2 | 17% |
| Unspecified | 1 | 8% |
| Other | 1 | 8% |
| Other | 0 | 0% |
| Unknown | 1 | 8% |
| Readers by discipline | Count | As % |
|---|---|---|
| Agricultural and Biological Sciences | 3 | 25% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 17% |
| Medicine and Dentistry | 2 | 17% |
| Biochemistry, Genetics and Molecular Biology | 1 | 8% |
| Unspecified | 1 | 8% |
| Other | 1 | 8% |
| Unknown | 2 | 17% |
Attention Score in Context
This research output has an Altmetric Attention Score of 3. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 16 July 2012.
All research outputs
#8,534,976
of 25,373,627 outputs
Outputs from Naunyn-Schmiedeberg's Archives of Pharmacology
#438
of 1,892 outputs
Outputs of similar age
#13,226
of 39,276 outputs
Outputs of similar age from Naunyn-Schmiedeberg's Archives of Pharmacology
#5
of 13 outputs
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So far Altmetric has tracked 1,892 research outputs from this source. They receive a mean Attention Score of 4.2. This one is in the 30th percentile – i.e., 30% of its peers scored the same or lower than it.
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