Document Detail

Tezosentan inhibits both equinatoxin II and endotelin-1 induced contractions of isolated porcine coronary artery in a similar way.
MedLine Citation:
PMID:  12182543     Owner:  NLM     Status:  MEDLINE    
In the present study we examined the endothelium-dependent mechanism in the constriction of the isolated porcine coronary artery induced by Equinatoxin II (EqT II). EqT II is a polypeptide isolated from the sea anemone (Actinia equina, L.). Contractions induced by endothelin-1 (ET-1) were compared with the contractions induced by EqT II. The force of contraction induced by 100 nM EqT II reached only 30% of the force of contraction induced by 100 nM ET-1. EC50 for ET-1 was 5.14 nM, and for EqT II 101.1 nM. The effects of tezosentan, an endothelin ETA/B receptor antagonist, on contractions induced by either ET-1 or EqT II were compared. Tezosentan inhibited both ET-1 and, to a lesser extent, EqT II-induced contractions of isolated porcine coronary artery. Our present results confirm the involvement of endothelium in the EqT II-induced contractions of coronary arteries. The mode of action of tezosentan upon EqT II-induced contractions indicate that besides its pore-forming effect in the membranes, endothelium, and specifically endothelin-dependent mechanisms, are very important components of the toxin constrictory effects.
Gorazd Drevensek; Simona Kirbis; Matjaz Bunc; Mojca Zitko; Metka V Budihna; Dusan Suput
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of natural toxins     Volume:  11     ISSN:  1058-8108     ISO Abbreviation:  J Nat Toxins     Publication Date:  2002 Aug 
Date Detail:
Created Date:  2002-08-16     Completed Date:  2003-03-10     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9208016     Medline TA:  J Nat Toxins     Country:  United States    
Other Details:
Languages:  eng     Pagination:  231-44     Citation Subset:  IM    
Institute of Pharmacology and Experimental Toxicology, Faculty of Medicine, University of Ljubljana, Slovenia.
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MeSH Terms
Cnidarian Venoms / pharmacology
Coronary Vessels / drug effects,  physiology*
Endothelin-1 / pharmacology
Endothelium / drug effects,  physiology
Marine Toxins / adverse effects*,  pharmacology
Pyridines / adverse effects*,  pharmacology
Receptors, Endothelin
Sea Anemones / chemistry*
Tetrazoles / adverse effects*,  pharmacology
Vasodilator Agents / adverse effects*,  pharmacology
Reg. No./Substance:
0/Cnidarian Venoms; 0/Endothelin-1; 0/Marine Toxins; 0/Pyridines; 0/Receptors, Endothelin; 0/Tetrazoles; 0/Vasodilator Agents; 0/tezosentan; 54578-46-0/equinatoxin

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