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X Demographics
Mendeley readers
Attention Score in Context
| Title |
Pharmacological Characterization of 5-Substituted 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazines: Novel Antagonists for the Histamine H3 and H4 Receptors with Anti-inflammatory Potential
|
|---|---|
| Published in |
Frontiers in Pharmacology, November 2017
|
| DOI | 10.3389/fphar.2017.00825 |
| Pubmed ID | |
| Authors |
Michelle F. Corrêa, Álefe J. R. Barbosa, Larissa B. Teixeira, Diego A. Duarte, Sarah C. Simões, Lucas T. Parreiras-e-Silva, Aleksandro M. Balbino, Richardt G. Landgraf, Michel Bouvier, Claudio M. Costa-Neto, João P. S. Fernandes |
| Abstract |
The histamine receptors (HRs) are traditional G protein-coupled receptors of extensive therapeutic interest. Recently, H3R and H4R subtypes have been targeted in drug discovery projects for inflammation, asthma, pain, cancer, Parkinson's, and Alzheimer's diseases, which includes searches for dual acting H3R/H4R ligands. In the present work, nine 1-[(2,3-dihydro-1-benzofuran-2-yl)methyl]piperazine (LINS01 series) molecules were synthesized and evaluated as H3R and H4R ligands. Our data show that the N-allyl-substituted compound LINS01004 bears the highest affinity for H3R (pKi 6.40), while the chlorinated compound LINS01007 has moderate affinity for H4R (pKi 6.06). In addition, BRET assays to assess the functional activity of Gi1 coupling indicate that all compounds have no intrinsic activity and act as antagonists of these receptors. Drug-likeness assessment indicated these molecules are promising leads for further improvements. In vivo evaluation of compounds LINS01005 and LINS01007 in a mouse model of asthma showed a better anti-inflammatory activity of LINS01007 (3 g/kg) than the previously tested compound LINS01005. This is the first report with functional data of these compounds in HRs, and our results also show the potential of their applications as anti-inflammatory. |
X Demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 37 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 37 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 6 | 16% |
| Student > Bachelor | 4 | 11% |
| Student > Master | 4 | 11% |
| Student > Doctoral Student | 3 | 8% |
| Researcher | 3 | 8% |
| Other | 5 | 14% |
| Unknown | 12 | 32% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 8 | 22% |
| Chemistry | 4 | 11% |
| Biochemistry, Genetics and Molecular Biology | 3 | 8% |
| Agricultural and Biological Sciences | 2 | 5% |
| Immunology and Microbiology | 1 | 3% |
| Other | 3 | 8% |
| Unknown | 16 | 43% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. 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 November 2017.
All research outputs
#20,452,930
of 23,008,860 outputs
Outputs from Frontiers in Pharmacology
#10,214
of 16,314 outputs
Outputs of similar age
#283,420
of 325,276 outputs
Outputs of similar age from Frontiers in Pharmacology
#157
of 261 outputs
Altmetric has tracked 23,008,860 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 16,314 research outputs from this source. They receive a mean Attention Score of 5.0. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 261 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.