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Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings.

López-Canales JS, Lozano-Cuenca J, Muãoz-Islas E, Aguilar-Carrasco JC, López-Canales OA, López-Mayorga RM, Castillo-Henkel EF, Valencia-Hernández I, Castillo-Henkel C - Braz. J. Med. Biol. Res. (2015)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Section of Postgraduate Studies and Investigation, Higher School of Medicine from the National Polytechnic Institute, Mexico City, Mexico.

ABSTRACT
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.

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Effects of 10-5 M cycloheximide on amfepramone-inducedvasorelaxation in rat aortic rings with functional endothelium andprecontracted with 10-6 M phenylephrine (PE). Data are reported asmeans±SE of n=6 observations. P>0.05 vs control (two-wayrepeated-measures ANOVA).
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f06: Effects of 10-5 M cycloheximide on amfepramone-inducedvasorelaxation in rat aortic rings with functional endothelium andprecontracted with 10-6 M phenylephrine (PE). Data are reported asmeans±SE of n=6 observations. P>0.05 vs control (two-wayrepeated-measures ANOVA).

Mentions: Figure 6 shows the effect of 10-5 Mcycloheximide on the relaxation induced by 10-9-10-5 Mamfepramone on phenylephrine-precontracted rat aortic rings. The maximum vasorelaxanteffect produced by amfepramone was unaffected by the presence (95.08±1.54%) orabsence (93.12±2.37%) of cycloheximide.


Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings.

López-Canales JS, Lozano-Cuenca J, Muãoz-Islas E, Aguilar-Carrasco JC, López-Canales OA, López-Mayorga RM, Castillo-Henkel EF, Valencia-Hernández I, Castillo-Henkel C - Braz. J. Med. Biol. Res. (2015)

Effects of 10-5 M cycloheximide on amfepramone-inducedvasorelaxation in rat aortic rings with functional endothelium andprecontracted with 10-6 M phenylephrine (PE). Data are reported asmeans±SE of n=6 observations. P>0.05 vs control (two-wayrepeated-measures ANOVA).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4470313&req=5

f06: Effects of 10-5 M cycloheximide on amfepramone-inducedvasorelaxation in rat aortic rings with functional endothelium andprecontracted with 10-6 M phenylephrine (PE). Data are reported asmeans±SE of n=6 observations. P>0.05 vs control (two-wayrepeated-measures ANOVA).
Mentions: Figure 6 shows the effect of 10-5 Mcycloheximide on the relaxation induced by 10-9-10-5 Mamfepramone on phenylephrine-precontracted rat aortic rings. The maximum vasorelaxanteffect produced by amfepramone was unaffected by the presence (95.08±1.54%) orabsence (93.12±2.37%) of cycloheximide.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Section of Postgraduate Studies and Investigation, Higher School of Medicine from the National Polytechnic Institute, Mexico City, Mexico.

ABSTRACT
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.

Show MeSH
Related in: MedlinePlus