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Type: Artigo de periódico
Title: Relaxing Effects Induced By The Soluble Guanylyl Cyclase Stimulator Bay 41-2272 In Human And Rabbit Corpus Cavernosum.
Author: Baracat, Juliana S
Teixeira, Cleber E
Okuyama, Cristina E
Priviero, Fernanda B M
Faro, Renato
Antunes, Edson
De Nucci, Gilberto
Abstract: 5-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.
Subject: Adolescent
Cyclic Amp
Drug Synergism
Enzyme Activators
Guanylate Cyclase
In Vitro Techniques
Isometric Contraction
Middle Aged
Muscle Relaxation
Ng-nitroarginine Methyl Ester
Nitric Oxide
Nitric Oxide Synthase
Citation: European Journal Of Pharmacology. v. 477, n. 2, p. 163-9, 2003-Sep.
Rights: fechado
Date Issue: 2003
Appears in Collections:Unicamp - Artigos e Outros Documentos

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