Literature DB >> 31710963

Relaxing effects of clenbuterol, ritodrine, salbutamol and fenoterol on the contractions of horse isolated bronchi induced by different stimuli.

Cristina Pozzoli1, Simone Bertini2, Enzo Poli1, Giuseppe Placenza2, Alessandro Menozzi3.   

Abstract

β2-adrenoceptor agonists are considered the most effective drugs to counteract bronchoconstriction in horses with asthma, but only clenbuterol is commonly employed in clinical practice. We evaluated the effects of different selective β2 agonists: clenbuterol, ritodrine, salbutamol, and fenoterol on the contractions of isolated bronchial muscle of horses induced by electrical field stimulation (EFS), carbachol, histamine, and KCl. All β2 agonists reduced the amplitude of contraction induced by the different stimuli but with variable efficacy and potency. Fenoterol and salbutamol were more effective than clenbuterol in relaxing the bronchial contractions induced by EFS and histamine, and were able to completely abolish carbachol-induced contractions, unlike clenbuterol and ritodrine. The respective potency values (pEC50) of clenbuterol, ritodrine, salbutamol, and fenoterol were 7.74 ± 0.20, 7.77 ± 0.17, 7.30 ± 0.23, 8.01 ± 0.13, for EFS-induced contractions; 8.39 ± 0.26, 5.49 ± 0.28, 6.63 ± 0.14, 7.68 ± 0.11, for carbachol-induced contraction; 7.39 ± 0.27, 7.04 ± 0.28, 6.45 ± 0.34, 7.34 ± 0.22, for histamine-induced contraction; 7.15 ± 0.06, 6.07 ± 0.20, 6.48 ± 0.14, 6.70 ± 0.18, for KCl-induced contraction. Salbutamol and fenoterol showed a higher efficacy than clenbuterol in relaxing horse bronchial muscle pre-contracted by most stimuli. Clenbuterol displayed a good potency but a rather low efficacy, and this may be due to its partial agonist nature; ritodrine showed lower or not significantly different efficacy and potency compared to the other agonists. An evaluation of the clinical efficacy by fenoterol and salbutamol in horses with asthma could be of great interest to assess if they could represent more effective bronchodilators compared to clenbuterol.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Bronchi; Clenbuterol; Fenoterol; Horse; Ritodrine; Salbutamol

Mesh:

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Year:  2019        PMID: 31710963     DOI: 10.1016/j.rvsc.2019.10.022

Source DB:  PubMed          Journal:  Res Vet Sci        ISSN: 0034-5288            Impact factor:   2.534


  1 in total

1.  Fenoterol and dobutamine as SARS-CoV-2 main protease inhibitors: A virtual screening study.

Authors:  Kayhan Bolelli; Tugba Ertan-Bolelli; Ozan Unsalan; Cisem Altunayar-Unsalan
Journal:  J Mol Struct       Date:  2020-10-13       Impact factor: 3.196

  1 in total

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