Distinct endothelin-B receptors mediate the effects of sarafotoxin S6c and IRL1620 in the ileum

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dc.contributor.author Miasiro, N. [UNIFESP]
dc.contributor.author Karaki, H.
dc.contributor.author Paiva, ACM [UNIFESP]
dc.date.accessioned 2016-01-24T12:30:30Z
dc.date.available 2016-01-24T12:30:30Z
dc.date.issued 1998-01-01
dc.identifier http://dx.doi.org/10.1097/00005344-199800001-00050
dc.identifier.citation Journal of Cardiovascular Pharmacology. Philadelphia: Lippincott Williams & Wilkins, v. 31, p. S175-S178, 1998.
dc.identifier.issn 0160-2446
dc.identifier.uri http://repositorio.unifesp.br/handle/11600/25834
dc.description.abstract In the guinea pig ileum, both sarafotoxin S6c (S6c) and IRL1620 induced a biphasic effect (relaxation and contraction). S6c induced strong tachyphylaxis of both components of the response, but IRL1620 induced tachyphylaxis mainly of the contractile component. Whereas the tissues rendered tachyphylactic to S6c did not respond to IRL1620, a normal biphasic response to S6c was observed in the tissues rendered tachyphylactic to IRL1620. in the presence of IRL1620, S6c could induce its biphasic effect, whereas in the presence of S6c, IRL1620 was ineffective. BQ-123, a specific ETA antagonist, did not affect the biphasic response induced by either agonist. PD145065, a potent ETA/ETB antagonist, was a competitive and a noncompetitive antagonist, respectively, of the contractile components of IRL1620 and S6c. RES-701-1, a specific ETB1 antagonist, inhibited both components of the response induced by IRL1620. However, it inhibited mainly the relaxant component induced by low doses of S6c. Apamin had different effects on endothelin-1 (ET-1), S6c, and IRL1620. Our results suggest that there are at least two distinct populations of ETB receptors mediating the biphasic response: the ETB1 receptor, sensitive to RES-701-1 and PD145065, and the ETB2 receptor, less sensitive to RES-701-1 and PD145065. en
dc.format.extent S175-S178
dc.language.iso eng
dc.publisher Lippincott Williams & Wilkins
dc.relation.ispartof Journal of Cardiovascular Pharmacology
dc.rights Acesso aberto
dc.subject sarafotoxin S6c en
dc.subject IRL1620 en
dc.subject ileum (guinea pig) en
dc.subject endothelin receptor subtypes en
dc.subject tachyphylaxis en
dc.title Distinct endothelin-B receptors mediate the effects of sarafotoxin S6c and IRL1620 in the ileum en
dc.type Artigo
dc.contributor.institution Universidade Federal de São Paulo (UNIFESP)
dc.contributor.institution Univ Tokyo
dc.description.affiliation Escola Paulista Med, Dept Biofis, BR-04023062 São Paulo, Brazil
dc.description.affiliation Univ Tokyo, Grad Sch Agr & Life Sci, Dept Vet Pharmacol, Tokyo, Japan
dc.description.affiliationUnifesp Escola Paulista Med, Dept Biofis, BR-04023062 São Paulo, Brazil
dc.identifier.doi 10.1097/00005344-199800001-00050
dc.description.source Web of Science
dc.identifier.wos WOS:000174051600050

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