Et-1 and Et-3 Actions Mediated by Cloned ETA Endothelin Receptors Exhibit Different Sensitivities to BQ-123

Et-1 and Et-3 activate phospholipase C in fibroblasts expressing cloned ETA receptors of bovine, rat and human origins. BQ-123 competitively antagonizes both responses but Et-3 actions are 10 times more sensitive to BQ-123 than Et-1 actions. It is suggested that differential sensitivity to BQ-123 is...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 1996-07, Vol.224 (1), p.169-171
Main Authors: Gresser, Olivia, Chayard, Denise, Herbert, Denis, Cousin, Marie Anne, Le Moullec, Jean Michel, Bouattane, Fatima, Guedin, Denis, Frelin, Christian
Format: Article
Language:English
Subjects:
Animals
Cattle
Cell Line
CHO Cells
Cloning, Molecular
Cricetinae
Dose-Response Relationship, Drug
Endothelin Receptor Antagonists
Endothelins - antagonists & inhibitors
Endothelins - pharmacology
Female
Humans
Kinetics
Peptides, Cyclic - pharmacology
Placenta - metabolism
Pregnancy
Rats
Receptor, Endothelin A
Receptors, Endothelin - biosynthesis
Receptors, Endothelin - physiology
Recombinant Proteins - drug effects
Recombinant Proteins - metabolism
Type C Phospholipases - metabolism
Uterus - metabolism
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Summary:Et-1 and Et-3 activate phospholipase C in fibroblasts expressing cloned ETA receptors of bovine, rat and human origins. BQ-123 competitively antagonizes both responses but Et-3 actions are 10 times more sensitive to BQ-123 than Et-1 actions. It is suggested that differential sensitivity to BQ-123 is an intrinsic property of Et-1 and Et-3 activated ETA receptors and that there is no need to postulate the existence of new ETA receptor isoforms to account for singular actions of BQ-123.
ISSN:0006-291X
1090-2104
DOI:10.1006/bbrc.1996.1002