Angiotensin receptor in the heart of Bothrops jararaca snake

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dc.contributor.authorBreno, M. C.
dc.contributor.authorPorto, C. S.
dc.contributor.authorPicarelli, Z. P.
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.contributor.institutionInst Butantan
dc.date.accessioned2016-01-24T12:31:21Z
dc.date.available2016-01-24T12:31:21Z
dc.date.issued2001-04-06
dc.description.abstractAngiotensin II interacts with specific cell surface angiotensin AT(1) and AT(2) receptors and, in some vertebrates, with an atypical angiotensin AT receptor. This study was designed to characterize the angiotensin receptor in the heart of Bothrops jararaca snake. A specific and saturable angiotensin II binding site was detected in cardiac membranes and yielded K-d = 7.34 +/- 1.41 nM and B-max = 72.49 +/- 18 fmol/mg protein. Competition-binding studies showed an angiotensin receptor with low affinity to both angiotensin receptor antagonists, losartan (2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole) and PD123319 ((s)-1-(4-[dimethylamino]-3-methylphenyl)methyl-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylate). Studies on the intracellular signaling pathways showed that phospholipase C/inositol phosphate breakdown and adenylylcyclase/cyclic AMP generation were not coupled with this angiotensin receptor. An adenylylcyclase enzyme sensitive to forskolin was detected. the results indicate the presence of an angiotensin receptor in the heart of B. jararaca snake pharmacologically distinct from angiotensin AT(1) and AT(2) receptors. It seems to belong to a new class of angiotensin receptors, like some other atypical angiotensin AT receptors that have already been described. (C) 2001 Elsevier Science B.V. All rights reserved.en
dc.description.affiliationUniversidade Federal de São Paulo, Escola Paulista Med, Dept Pharmacol, Sect Expt Endocrinol, BR-04044020 São Paulo, Brazil
dc.description.affiliationInst Butantan, Pharmacol Lab, São Paulo, Brazil
dc.description.affiliationUnifespUniversidade Federal de São Paulo, Escola Paulista Med, Dept Pharmacol, Sect Expt Endocrinol, BR-04044020 São Paulo, Brazil
dc.description.sourceWeb of Science
dc.format.extent27-35
dc.identifierhttp://dx.doi.org/10.1016/S0014-2999(01)00894-9
dc.identifier.citationEuropean Journal of Pharmacology. Amsterdam: Elsevier B.V., v. 417, n. 1-2, p. 27-35, 2001.
dc.identifier.doi10.1016/S0014-2999(01)00894-9
dc.identifier.issn0014-2999
dc.identifier.urihttp://repositorio.unifesp.br/handle/11600/26527
dc.identifier.wosWOS:000168220400004
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofEuropean Journal of Pharmacology
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.rights.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.subjectangiotensin receptoren
dc.subjectangiotensin AT(1) receptor-selective antagonisten
dc.subjectangiotensin AT(2) receptor-selective antagonisten
dc.subjectinositol phosphateen
dc.subjectadenylylcyclase forskolin-sensitiveen
dc.subjecthearten
dc.titleAngiotensin receptor in the heart of Bothrops jararaca snakeen
dc.typeinfo:eu-repo/semantics/article
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