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Article (Scientific journals)
Endothelins: functional and autoradiographic studies in guinea pig trachea
Tschirhart, Eric; Drijfhout, J. W.; Pelton, J. T. et al.
1991In Journal of Pharmacology and Experimental Therapeutics, 258 (1), p. 381-7
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Keywords :
Animals; pharmacology; metabolism; Trachea; Muscle, Smooth; Muscle Contraction; Male; Guinea Pigs; Glycopeptides; Epithelium; Endothelins; Drug Interactions; Binding Sites; Autoradiography; Anti-Bacterial Agents; drug effects
Abstract :
[en] The presence of binding sites for [125I]endothelin-1 and the contractile activities of endothelins (ETs) and sarafotoxin S6b and the endothelin fragment ET(16-21) were investigated in guinea pig trachea. ETs and sarafotoxin S6b (0.1-100 nM) induced potent contractile responses in guinea pig trachea with EC50 values ranging from 1.57 to 12.97 nM. Epithelium removal increased the potencies of ET-1, ET-2 and S6b, but not that of ET-3, and maximal responses to ET-1 and ET-2 were also increased. Effects of epithelium removal were partially mimicked by phosphoramidon (10 microM), an enkephalinase inhibitor, suggesting that enkephalinase (EC.3.4.24.11.) is able to degrade ET-1 and ET-2. ET-3-induced contractions were not affected by phosphoramidon. Autoradiographic studies suggested the presence of at least two specific binding sites for [125]ET-1 in guinea pig airway smooth muscle. The correlation between Kd and EC50 values suggests that the binding sites identified in the airway smooth muscle represent functional receptors for ETs. ET(16-21) and ET(16-21)-NH2 were less potent agonists than the ETs in guinea pig trachea and 10 microM ET(16-21) was unable to inhibit [125I]ET-1 binding in guinea pig airway smooth muscle. Therefore, these results suggest that the C-terminal hexapeptide of ET-1 cannot be used to classify ET receptors in guinea pig trachea.
Disciplines :
Biochemistry, biophysics & molecular biology
Identifiers :
UNILU:UL-ARTICLE-2008-218
Author, co-author :
Tschirhart, Eric ;  University of Luxembourg > Faculty of Science, Technology and Communication (FSTC) > Life Science Research Unit
Drijfhout, J. W.
Pelton, J. T.
Miller, R. C.
Jones, C. R.
Language :
English
Title :
Endothelins: functional and autoradiographic studies in guinea pig trachea
Publication date :
1991
Journal title :
Journal of Pharmacology and Experimental Therapeutics
ISSN :
1521-0103
Publisher :
American Society for Pharmacology and Experimental Therapeutics, Bethesda, United States - Maryland
Volume :
258
Issue :
1
Pages :
381-7
Peer reviewed :
Peer Reviewed verified by ORBi
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since 09 September 2013

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