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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