β-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 β 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 β 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 (pEC) 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.
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http://dx.doi.org/10.1016/j.rvsc.2019.10.022 | DOI Listing |
Res Vet Sci
February 2020
Department of Veterinary Science, University of Parma, Strada del Taglio 10, 43126 Parma, Italy. Electronic address:
β-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 β 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 β agonists reduced the amplitude of contraction induced by the different stimuli but with variable efficacy and potency.
View Article and Find Full Text PDFFood Chem
February 2016
State Key Laboratory of Animal Nutrition, College of Animal Science and Technology, China Agricultural University, Beijing 100193, PR China. Electronic address:
Broad screening and identification of β-agonists in feed, serum, urine, muscle and liver samples was achieved in a quick and highly sensitive manner using ultra high performance liquid chromatography-quadrupole-orbitrap high resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS) combined with a spectra library search. Solid-phase extraction technology was employed for sample purification and enrichment. After extraction and purification, the samples were analyzed using a Q-Orbitrap high-resolution mass spectrometer under full-scan and data-dependent MS/MS mode.
View Article and Find Full Text PDFA new method has been developed using a hybrid triple-quadrupole linear ion trap (QTrap) mass spectrometer for the fast detection and identification of nine beta-agonists, clenbuterol, salbutamol, ractopamine, ritodrine, terbutaline, isoxsuprine, tulobuterol, cimaterol and bambuterol, in one single liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. The homogenized tissue samples were purified with liquid-liquid extraction after enzymatic hydrolysis by P-glucuronidase/aryl sulfatase. After gradient elution separation on C(18) LC column using acetonitrile and formic acid aqueous solution as the mobile phases, a multiple reaction monitoring (MRM) scan as survey scan and an enhanced product ion (EPI) scan as dependent scan were performed in an information dependent acquisition (IDA) experiment.
View Article and Find Full Text PDFBiomed Chromatogr
April 2010
Centro Regionale di Tossicologia della Regione Piemonte, Consorzio Antidoping A. Bertinaria, Regione Gonzole 10/1, Orbassano, Turin, Italy.
A fast screening protocol was developed and validated for the simultaneous determination of 15 beta(2)-agonists in human urine (bambuterol, cimbuterol, clenbuterol, fenoterol, formoterol, isoproterenol, mapenterol, metaproterenol, procaterol, ractopamine, ritodrine, salbutamol, salmeterol, terbutaline, tulobuterol). The overall sample processing includes deconjugation with enzyme hydrolysis, liquid-liquid extraction, followed by derivatization of the extract and detection of beta(2)-agonists trimethylsilyl-derivatives by fast-gas chromatography/electron impact-mass spectrometry (fast-GC/EI-MS). Sample extraction and derivatization were optimized with the purpose of improving recoveries and reaction yields for a variety of analytes with different structures simultaneously, while keeping the procedure simple and reliable.
View Article and Find Full Text PDFRecent Pat CNS Drug Discov
November 2009
Institute of Cellular and Integrative Neurosciences, Centre National de la Recherche Scientifique, Strasbourg, France.
The market for pain treatment is a major segment of nervous system pathologies. Despite this dynamism, the management of some pain conditions remains a clinical challenge. Neuropathic pain arises as a direct consequence of a lesion or disease affecting the somatosensory system.
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