Evidence for two atypical conformations of beta-adrenoceptors and their interaction with Gi proteins

dc.creatorSantos, IN
dc.creatorSumitame, M
dc.creatorCaceres, VA
dc.creatorMoreira, MF
dc.creatorKrieger, MH
dc.creatorSpadari-Bratfisch, RC
dc.date2005
dc.dateAPR 18
dc.date2014-11-17T09:48:10Z
dc.date2015-11-26T17:23:00Z
dc.date2014-11-17T09:48:10Z
dc.date2015-11-26T17:23:00Z
dc.date.accessioned2018-03-29T00:10:22Z
dc.date.available2018-03-29T00:10:22Z
dc.identifierEuropean Journal Of Pharmacology. Elsevier Science Bv, v. 513, n. 41671, n. 109, n. 118, 2005.
dc.identifier0014-2999
dc.identifierWOS:000229362000012
dc.identifier10.1016/j.ejphar.2005.03.008
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/66095
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/66095
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/66095
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1283729
dc.descriptionIn this study, we investigated whether the responses of right atria from sinoaortic denervated rats to CGP12177 (4(3-t-butylamino-2-hydroxypropoxy benzidimidazole-2 one, hydrochloride)), isoprenaline and norepinephrine desensitized in parallel and whether CGP12177 interacted with distinct conformations of beta-adrenoceptors. Right atria from rats 48 h after sinoaortic denervation were subsensitive to isoprenaline, norepinephrine and CGP12177. One week after sinoaortic denervation, the sensitivity to CGP12177 had recovered whereas the responses to isoprenaline and norepinephrine were still subsensitive, suggesting that the binding sites for these molecules showed independent behavior. In atria from 48 h sinoaortic-denervated rats, propranolol or 3 mu M CGP20712A (2-hydroxy-5(2-((2-hydroxy-3-(4((methyl-4-trifluormethyl)1H imidazole-2-yl)-phenoxypropyl) amino) ethoxy)-benzamide monomethane sulphonate)) blocked the responses to 10 nM-1 mu M CGP12177 and steepened the curves. The concentration-response curves to CGP12177 in the presence of 10118,551 (erythro-DL-1(-methylindan-4-yloxy)-3-isopropylamino-butan-2-ol) were biphasic, suggesting that CGP12177 interacted with at least two conforinations of beta-adrenoceptors that showed negative cooperativism, one acting through beta(2)-adrenoceptor-Gi and the other via adrenoceptor-Gs. This hypothesis was confirmed in right atria from sinoaortic-denervated rats treated with pertussis toxin. (c) 2005 Elsevier B.V. All rights reserved.
dc.description513
dc.description41671
dc.description109
dc.description118
dc.languageen
dc.publisherElsevier Science Bv
dc.publisherAmsterdam
dc.publisherHolanda
dc.relationEuropean Journal Of Pharmacology
dc.relationEur. J. Pharmacol.
dc.rightsfechado
dc.rightshttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.sourceWeb of Science
dc.subjectbeta(1)-adrenoceptor
dc.subjectbeta(4)-adrenoceptor
dc.subjectsinoaortic denervation
dc.subjectCGP12177
dc.subjectIsolated Rat-heart
dc.subjectEstrous-cycle
dc.subjectRight Atria
dc.subjectBeta(1)-adrenergic Receptors
dc.subjectDissociation-constants
dc.subjectChronotropic Response
dc.subjectAdrenergic-receptors
dc.subjectRelative Efficacies
dc.subjectContractile-force
dc.subjectStressed Rats
dc.titleEvidence for two atypical conformations of beta-adrenoceptors and their interaction with Gi proteins
dc.typeArtículos de revistas


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