Comparative study of sildenafil analogues in the rabbit isolated aorta (2005)
- Authors:
- Autor USP: NUCCI, GILBERTO DE - ICB
- Unidade: ICB
- Assunto: FARMACOLOGIA
- Language: Português
- Abstract: Objetivo: Sildenafil (SILD), which is a cGMP-specific PDE5 inhibitor, is used for the treatment of erectile dysfunction. Inhibition of PDE5 also relaxes vascular tissues. We developed 3 new analogue molecules of SILD (SILD-6, SILD-7 and SILD-8) in order to investigate others PDE5 inhibitors that could be more selective, potent and with less side effects than SILD. This work aimed to compare the relaxing effects of SILD- and SILD-6, 7 and 8 in rabbit aorta (RbA). Métodos e Resultados: Thoracic RbA was isolated and cut in rings. Aortic rings (AR) were mounted in organ baths filled with Krebs Solution. Tension was recorded using a isometric transducer connected to a PowerLab. Concentration-response curves (CRC) to SILD, SILD-6, SILD-7 and SILD-8 (1 nM to 10 jM) were constructed in endothelium intact (E+) and endothelium-denuded aortic rings (E-). SILD-6, SILD-7 and SILD-8 caused a concentration-dependent relaxation in AR. In the E+, the potencies (pEC50) for SILD-6 (6.94 ± 0.09), SILD-7 (6.97 ± 0.06) and SILD-8 (7.03 ± 0.08) were similar to the pEC50 for SILD (7.25 ± 0.07). Endothelium denudation caused a rightward shift in the CRC for SILD-6, SILD-7 and SILD-8 (pEC50: 6.55 ± 0.08; 6.46 ± 0.14; 6.57 ± 0.08, respectively) which was similar to the displacement for SILD (pEC50: 6.41 ± 0.12). In the E+, the maximal responses (EMAX) for SILD-6 (71 ± 2%), SILD-7 (74 ± 3%) and SILD-8 (71 ± 4%) were similar to EMAX for SILD (76 ± 8%). In the E-, the EMAX were similarlydiminished for SILD (35 ± 2%), SILD-6 (51 ± 7%), SILD-7 (45 ± 5) and SILD- 8 (51 ± 5%). Conclusões: In the RbA, sildenafil analogues (SILD-6, SILD-7 and SILD-8) evoked relaxations by a mechanism partially endothelium-dependent which was not distinct from SILD.
- Imprenta:
- Publisher: Federação de Sociedades de Biologia Experimental
- Publisher place: Águas de Lindóia, São Paulo
- Date published: 2005
- Source:
- Título: Resumos
- Conference titles: Reunião Anual da Federação de Sociedades de Biologia Experimental, FeSBE
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ABNT
FLORES, H. A. et al. Comparative study of sildenafil analogues in the rabbit isolated aorta. 2005, Anais.. Águas de Lindóia, São Paulo: Federação de Sociedades de Biologia Experimental, 2005. . Acesso em: 18 nov. 2024. -
APA
Flores, H. A., Priviero, F. B. M., Teixeira, C. E., Antunes, E., & De Nucci, G. (2005). Comparative study of sildenafil analogues in the rabbit isolated aorta. In Resumos. Águas de Lindóia, São Paulo: Federação de Sociedades de Biologia Experimental. -
NLM
Flores HA, Priviero FBM, Teixeira CE, Antunes E, De Nucci G. Comparative study of sildenafil analogues in the rabbit isolated aorta. Resumos. 2005 ;[citado 2024 nov. 18 ] -
Vancouver
Flores HA, Priviero FBM, Teixeira CE, Antunes E, De Nucci G. Comparative study of sildenafil analogues in the rabbit isolated aorta. Resumos. 2005 ;[citado 2024 nov. 18 ] - Presence of nitric oxide synthase inhibitor activity in rat pleural exsudates
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