Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings
Amfepramone (diethylpropion) is an appetite-suppressant drug used for the treatment of overweight and obesity. It has been suggested that the systemic and central activity of amfepramone produces cardiovascular effects such as transient ischemic attacks and primary pulmonary hypertension. However, i...
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| Format: | Article |
| Language: | English |
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Associação Brasileira de Divulgação Científica
2015-03-01
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| Series: | Brazilian Journal of Medical and Biological Research |
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| Online Access: | http://www.scielo.br/pdf/bjmbr/v48n6/1414-431X-bjmbr-1414-431X20144261.pdf |
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| author | J.S. López-Canales J. Lozano-Cuenca E. Muãoz-Islas J.C. Aguilar-Carrasco O.A. López-Canales R.M. López-Mayorga E.F. Castillo-Henkel I. Valencia-Hernández C. Castillo-Henkel |
| author_facet | J.S. López-Canales J. Lozano-Cuenca E. Muãoz-Islas J.C. Aguilar-Carrasco O.A. López-Canales R.M. López-Mayorga E.F. Castillo-Henkel I. Valencia-Hernández C. Castillo-Henkel |
| author_sort | J.S. López-Canales |
| collection | DOAJ |
| description | Amfepramone (diethylpropion) is an appetite-suppressant drug used for the treatment of overweight and obesity. It has been suggested that the systemic and central activity of amfepramone produces cardiovascular effects such as transient ischemic attacks and primary pulmonary hypertension. However, it is not known whether amfepramone produces immediate vascular effects when applied in vitro to rat aortic rings and, if so, what mechanisms may be involved. We analyzed the effect of amfepramone on phenylephrine-precontracted rat aortic rings with or without endothelium and the influence of inhibitors or blockers on this effect. Amfepramone produced a concentration-dependent vasorelaxation in phenylephrine-precontracted rat aortic rings that was not affected by the vehicle, atropine, 4-AP, glibenclamide, indomethacin, clotrimazole, or cycloheximide. The vasorelaxant effect of amfepramone was significantly attenuated by NG-nitro-L-arginine methyl ester (L-NAME) and tetraethylammonium (TEA), and was blocked by removal of the vascular endothelium. These results suggest that amfepramone had a direct vasorelaxant effect on phenylephrine-precontracted rat aortic rings, and that inhibition of endothelial nitric oxide synthase and the opening of Ca2+-activated K+ channels were involved in this effect. |
| first_indexed | 2024-04-11T15:08:49Z |
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| id | doaj.art-c42a6b2c0f3f41d1b89bd7440ae43f02 |
| institution | Directory Open Access Journal |
| issn | 1414-431X |
| language | English |
| last_indexed | 2024-04-11T15:08:49Z |
| publishDate | 2015-03-01 |
| publisher | Associação Brasileira de Divulgação Científica |
| record_format | Article |
| series | Brazilian Journal of Medical and Biological Research |
| spelling | doaj.art-c42a6b2c0f3f41d1b89bd7440ae43f022022-12-22T04:16:43ZengAssociação Brasileira de Divulgação CientíficaBrazilian Journal of Medical and Biological Research1414-431X2015-03-0148653754410.1590/1414-431x20144261Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic ringsJ.S. López-CanalesJ. Lozano-CuencaE. Muãoz-IslasJ.C. Aguilar-CarrascoO.A. López-CanalesR.M. López-MayorgaE.F. Castillo-HenkelI. Valencia-HernándezC. Castillo-HenkelAmfepramone (diethylpropion) is an appetite-suppressant drug used for the treatment of overweight and obesity. It has been suggested that the systemic and central activity of amfepramone produces cardiovascular effects such as transient ischemic attacks and primary pulmonary hypertension. However, it is not known whether amfepramone produces immediate vascular effects when applied in vitro to rat aortic rings and, if so, what mechanisms may be involved. We analyzed the effect of amfepramone on phenylephrine-precontracted rat aortic rings with or without endothelium and the influence of inhibitors or blockers on this effect. Amfepramone produced a concentration-dependent vasorelaxation in phenylephrine-precontracted rat aortic rings that was not affected by the vehicle, atropine, 4-AP, glibenclamide, indomethacin, clotrimazole, or cycloheximide. The vasorelaxant effect of amfepramone was significantly attenuated by NG-nitro-L-arginine methyl ester (L-NAME) and tetraethylammonium (TEA), and was blocked by removal of the vascular endothelium. These results suggest that amfepramone had a direct vasorelaxant effect on phenylephrine-precontracted rat aortic rings, and that inhibition of endothelial nitric oxide synthase and the opening of Ca2+-activated K+ channels were involved in this effect.http://www.scielo.br/pdf/bjmbr/v48n6/1414-431X-bjmbr-1414-431X20144261.pdfCardiovascular pharmacologyAmfepramoneObesityRat aortaNitric oxidePotassium channels |
| spellingShingle | J.S. López-Canales J. Lozano-Cuenca E. Muãoz-Islas J.C. Aguilar-Carrasco O.A. López-Canales R.M. López-Mayorga E.F. Castillo-Henkel I. Valencia-Hernández C. Castillo-Henkel Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings Brazilian Journal of Medical and Biological Research Cardiovascular pharmacology Amfepramone Obesity Rat aorta Nitric oxide Potassium channels |
| title | Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings |
| title_full | Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings |
| title_fullStr | Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings |
| title_full_unstemmed | Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings |
| title_short | Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings |
| title_sort | mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings |
| topic | Cardiovascular pharmacology Amfepramone Obesity Rat aorta Nitric oxide Potassium channels |
| url | http://www.scielo.br/pdf/bjmbr/v48n6/1414-431X-bjmbr-1414-431X20144261.pdf |
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