2 RECEPTOR SUBTYPES ARE INVOLVED in the CONTRACTILE COMPONENT of the GUINEA-PIG ILEUM RESPONSES TO ENDOTHELINS

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dc.contributor.author Miasiro, N. [UNIFESP]
dc.contributor.author Paiva, ACM [UNIFESP]
dc.contributor.author Ihara, M.
dc.contributor.author Yano, M.
dc.date.accessioned 2016-01-24T11:40:10Z
dc.date.available 2016-01-24T11:40:10Z
dc.date.issued 1993-01-01
dc.identifier http://dx.doi.org/10.1097/00005344-199322008-00057
dc.identifier.citation Journal of Cardiovascular Pharmacology. Philadelphia: Lippincott-raven Publ, v. 22, p. S211-S213, 1993.
dc.identifier.issn 0160-2446
dc.identifier.uri http://repositorio.unifesp.br/handle/11600/25294
dc.description.abstract Endothelin-I (ET-1) and endothelin-3 (ET-3) induced a biphasic response (relaxation and contraction) in the guinea pig ileum. Short-term activation of protein kinase C (PKC) with phorbol 12,13-dibutyrate (PDBu) inhibited the contractile but not the relaxing component of the responses, as did H-7. Long-term pretreatment with PDBu reversed the short-term inhibition but did not affect the tachyphylaxis induced by ET-1. These results suggest that PKC contributes to ET-1 contraction but not to tachyphylaxis. the ETA antagonist BQ- 123, at 34 nM, competitively inhibited ET-1 contraction, but at 340 nM the inhibition was noncompetitive. Dose-response curves for ET-1 relaxation were shifted to the left. for ET-3, BQ-123 (340 nM) only decreased the maximal contractile response of the dose-response curve without affecting the relaxation. We suggest that in this tissue there is one receptor for ET-1-induced contraction, which is competitively antagonized by BQ-123, and another one for ET-3-induced contraction, which is noncompetitively antagonized by BQ-123. en
dc.format.extent S211-S213
dc.language.iso eng
dc.publisher Lippincott-raven Publ
dc.relation.ispartof Journal of Cardiovascular Pharmacology
dc.rights Acesso aberto
dc.subject ENDOTHELIN-1 en
dc.subject ENDOTHELIN-3 en
dc.subject RECEPTOR SUBTYPES en
dc.subject ENDOTHELIN ANTAGONIST en
dc.subject TACHYPHYLAXIS en
dc.title 2 RECEPTOR SUBTYPES ARE INVOLVED in the CONTRACTILE COMPONENT of the GUINEA-PIG ILEUM RESPONSES TO ENDOTHELINS en
dc.type Artigo
dc.contributor.institution BANYU PHARMACEUT CO LTD
dc.contributor.institution Universidade Federal de São Paulo (UNIFESP)
dc.description.affiliation BANYU PHARMACEUT CO LTD,TSUKUBA RES INST,TSUKUBA,JAPAN
dc.identifier.doi 10.1097/00005344-199322008-00057
dc.description.source Web of Science
dc.identifier.wos WOS:A1993MN02800057



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