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Developing anticholinergic drugs for the treatment of asthma with improved efficacy

Wong et al. | Jul 05, 2023

Developing anticholinergic drugs for the treatment of asthma with improved efficacy
Image credit: Wong et al.

Anticholinergics are used in treating asthma, a chronic inflammation of the airways. These drugs block human M1 and M2 muscarinic acetylcholine receptors, inhibiting bronchoconstriction. However, studies have reported complications of anticholinergic usage, such as exacerbated eosinophil production and worsened urinary retention. Modification of known anticholinergics using bioisosteric replacements to increase efficacy could potentially minimize these complications. The present study focuses on identifying viable analogs of anticholinergics to improve binding energy to the receptors compared to current treatment options. Glycopyrrolate (G), ipratropium (IB), and tiotropium bromide (TB) were chosen as parent drugs of interest, due to the presence of common functional groups within the molecules, specifically esters and alcohols. Docking score analysis via AutoDock Vina was used to evaluate the binding energy between drug analogs and the muscarinic acetylcholine receptors. The final results suggest that G-A3, IB-A3, and TB-A1 are the most viable analogs, as binding energy was improved when compared to the parent drug. G-A4, IB-A4, IB-A5, TB-A3, and TB-A4 are also potential candidates, although there were slight regressions in binding energy to both muscarinic receptors for these analogs. By researching the effects of bioisosteric replacements of current anticholinergics, it is evident that there is a potential to provide asthmatics with more effective treatment options.

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Pollination Patterns by Green-Backed Firecrown Hummingbirds

Freeland et al. | May 28, 2020

Pollination Patterns by Green-Backed Firecrown Hummingbirds

The Green-backed Firecrown hummingbird is an essential pollinator in the temperate rainforests of southern South America. However, little is known about the ecology of these birds. Authors examined the foraging patterns of these birds identifying interesting differences in foraging patterns among season, age and sex.

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On the Relationship Between Viscosity and Surface Tension

Wei et al. | Sep 16, 2014

On the Relationship Between Viscosity and Surface Tension

Surface tension and viscosity are both measures of how "sticky" a liquid is, but are they related? The authors here investigate the surface tension and viscosity of mixtures of water with different concentrations of agar agar, flour, or detergent. Surprisingly, they find that the least viscous mixtures had the strongest surface tensions, indicating that the two properties are not linked.

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