Relaxing Effects Induced By The Soluble Guanylyl Cyclase Stimulator Bay 41-2272 In Human And Rabbit Corpus Cavernosum.

dc.creatorBaracat, Juliana S
dc.creatorTeixeira, Cleber E
dc.creatorOkuyama, Cristina E
dc.creatorPriviero, Fernanda B M
dc.creatorFaro, Renato
dc.creatorAntunes, Edson
dc.creatorDe Nucci, Gilberto
dc.date2003-Sep
dc.date2015-11-27T12:52:28Z
dc.date2015-11-27T12:52:28Z
dc.date.accessioned2018-03-29T00:58:05Z
dc.date.available2018-03-29T00:58:05Z
dc.identifierEuropean Journal Of Pharmacology. v. 477, n. 2, p. 163-9, 2003-Sep.
dc.identifier0014-2999
dc.identifier
dc.identifierhttp://www.ncbi.nlm.nih.gov/pubmed/14519420
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/195547
dc.identifier14519420
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1295780
dc.description5-Cyclopropyl-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-pyrimidin-4-ylamine (BAY 41-2272) is a potent soluble guanylyl cyclase stimulator in a nitric oxide (NO)-independent manner. The relaxant effect of BAY 41-2272 was investigated in rabbit and human corpus cavernosum in vitro. BAY 41-2272 (0.01-10 microM) relaxed both rabbit (pEC(50)=6.82+/-0.06) and human (pEC(50)=6.12+/-0.10) precontracted cavernosal strips. The guanylyl cyclase inhibitor (ODQ, 10 microM) caused significant rightward shifts in the concentration-response curves for BAY 41-2272 in rabbit (4.7-fold) and human (2.3-fold) tissues. The NO synthesis inhibitor (N-nitro-L-arginine methyl ester (L-NAME), 100 microM) also produced similar rightward shifts, revealing that BAY 41-2272 acts synergistically with endogenous NO to elicit its relaxant effect. The results also indicate that ODQ is selective for the NO-stimulated enzyme, since relaxations evoked by BAY 41-2272 were only partly attenuated by ODQ. The present study shows that both BAY 41-2272 and sildenafil evoke relaxations independent of inhibition of haem in soluble guanylate cyclase. Moreover, there is no synergistic effect of the two compounds in corpus cavernosum.
dc.description477
dc.description163-9
dc.languageeng
dc.relationEuropean Journal Of Pharmacology
dc.relationEur. J. Pharmacol.
dc.rightsfechado
dc.rights
dc.sourcePubMed
dc.subjectAdolescent
dc.subjectAdult
dc.subjectAged
dc.subjectAnimals
dc.subjectCyclic Amp
dc.subjectDrug Synergism
dc.subjectEnzyme Activators
dc.subjectGuanylate Cyclase
dc.subjectHumans
dc.subjectIn Vitro Techniques
dc.subjectIsometric Contraction
dc.subjectMale
dc.subjectMiddle Aged
dc.subjectMuscle Relaxation
dc.subjectNg-nitroarginine Methyl Ester
dc.subjectNitric Oxide
dc.subjectNitric Oxide Synthase
dc.subjectOxadiazoles
dc.subjectPenis
dc.subjectPyrazoles
dc.subjectPyridines
dc.subjectRabbits
dc.titleRelaxing Effects Induced By The Soluble Guanylyl Cyclase Stimulator Bay 41-2272 In Human And Rabbit Corpus Cavernosum.
dc.typeArtículos de revistas


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