ENDOTHELIN (16-21) - BIPHASIC EFFECT AND NO DESENSITIZATION ON THE GUINEA-PIG ISOLATED ILEUM

ENDOTHELIN (16-21) - BIPHASIC EFFECT AND NO DESENSITIZATION ON THE GUINEA-PIG ISOLATED ILEUM

Author Miasiro, N. Google Scholar
Nakaie, Clovis Ryuichi Autor UNIFESP Google Scholar
Paiva, Antonio Cechelli de Mattos Autor UNIFESP Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Abstract 1 In the guinea-pig ileum the C-terminal hexapeptide of the endothelins, endothelin (16-21), induced a biphasic effect (relaxation followed by contraction) qualitatively similar to that seen in the responses to endothelins 1 and 3. Both components of the response were concentration-dependent in the range studied (2-100 mum).2 The response induced by endothelin (16-21) was inhibited in low-sodium (80mM) medium.3 Repeated administration of endothelin (16-21) induced no desensitization of the preparation, contrasting with the tachyphylaxis induced by endothelin-I and endothelin-3 in the guinea-pig ileum.4 Tissues rendered tachyphylatic to endothelin-1 or endothelin-3 responded normally to endothelin (16-21).5 The results suggest that the C-terminal tail of the endothelins contains the message for the biphasic response, whereas the N-terminal domain may be responsible for the strong binding to the receptor and for the tachyphylactic properties of endothelin-I and endothelin-3, in the guinea-pig isolated ileum. However, the possibility that endothelin (16-21) may be acting on a site other than the endothelin receptor cannot be ruled out.
Keywords ENDOTHELIN (16-21)
ENDOTHELIN-1
ENDOTHELIN-3
GUINEA-PIG ILEUM
DESENSITIZATION
SODIUM IONS
Language English
Date 1993-05-01
Published in British Journal Of Pharmacology. Basingstoke: Stockton Press, v. 109, n. 1, p. 68-72, 1993.
ISSN 0007-1188 (Sherpa/Romeo, impact factor)
Publisher Stockton Press
Extent 68-72
Origin http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.1993.tb13532.x/full
Access rights Open access Open Access
Type Article
Web of Science ID WOS:A1993KY99300011
URI http://repositorio.unifesp.br/11600/43176

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