New 8-substituted xanthiene derivatives as potent bronchodilators
Il Farmaco, ISSN: 0014-827X, Vol: 60, Issue: 11, Page: 974-980
2005
- 22Citations
- 13Captures
Metric Options: CountsSelecting the 1-year or 3-year option will change the metrics count to percentiles, illustrating how an article or review compares to other articles or reviews within the selected time period in the same journal. Selecting the 1-year option compares the metrics against other articles/reviews that were also published in the same calendar year. Selecting the 3-year option compares the metrics against other articles/reviews that were also published in the same calendar year plus the two years prior.
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations22
- Citation Indexes22
- 22
- CrossRef13
- Captures13
- Readers13
- 13
Article Description
The synthesis and structure determination of 8-aryl /alkyl aryl 1, 3-dimethyl-3, 7-dihydropurin-2, 6-dione derivatives (1-13), was carried out in this study. Bronchodilator activity is investigated using isolated guinea-pig tracheal strips, pre-contracted by acetylcholine and histamine. Spasmolytic activity of the compounds was compared to theophylline. Synthesized compounds (1-13) did not inhibit the acetylcholine-induced pre-contractions except compound (8) at 10 −5 M concentration. In contrast, some of the compounds, especially (7), (11), (12) at 10 −5 M and (3), (4), (9) and (11) in 10 −4 M displayed inhibitory activity on the tracheal strips pre-contracted by histamine. The potency of the compounds at human adenosine receptors was evaluated using radioligand binding assay and a cyclic AMP functional assay in CHO cells expressing these receptors. Compound (11) displayed the greatest activity against radioligand binding of specific agonists to A 2 A and A 2B receptors. The compounds were relatively selective for both A 2 A and A 2B compared with A 1 and A 3 receptors. All compounds were also tested for the inhibition of NECA-induced cAMP accumulation mediated by the A 2B adenosine receptor and compound (11) was found to be the most effective. Our results showed that these compounds are acting as selective adenosine antagonists, especially for adenosine A 2B receptors, and are promising as potent anti-inflammatory agents rather than bronchodilator for the treatment of asthma.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0014827X05001904; http://dx.doi.org/10.1016/j.farmac.2005.08.011; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=27744592938&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/16243321; https://linkinghub.elsevier.com/retrieve/pii/S0014827X05001904; https://dx.doi.org/10.1016/j.farmac.2005.08.011
Elsevier BV
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