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Mechanisms involved in the vasorelaxant effects produced by the acute application of amfepramone in vitro to rat aortic rings
- Source :
- Brazilian Journal of Medical and Biological Research, Volume: 48, Issue: 6, Pages: 537-544, Published: 27 MAR 2015, Brazilian Journal of Medical and Biological Research v.48 n.6 2015, Brazilian Journal of Medical and Biological Research, Associação Brasileira de Divulgação Científica (ABDC), instacron:ABDC, Scopus-Elsevier, Brazilian Journal of Medical and Biological Research, Vol 48, Iss 6, Pp 537-544 (2015)
- Publication Year :
- 2015
- Publisher :
- Associação Brasileira de Divulgação Científica, 2015.
-
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.
- Subjects :
- Male
Medicine (General)
Physiology
Vasodilator Agents
Amfepramone
Aorta, Thoracic
Pharmacology
Biochemistry
Glibenclamide
chemistry.chemical_compound
Phenylephrine
Vasoconstrictor Agents
General Pharmacology, Toxicology and Pharmaceutics
Biology (General)
lcsh:QH301-705.5
lcsh:R5-920
General Neuroscience
Tetraethylammonium
General Medicine
Potassium channel
Vasodilation
Atropine
medicine.anatomical_structure
NG-Nitroarginine Methyl Ester
Diethylpropion
lcsh:Medicine (General)
medicine.drug
medicine.medical_specialty
Endothelium
Nitric Oxide Synthase Type III
QH301-705.5
Immunology
Biophysics
Rat aorta
Ocean Engineering
Nitric oxide
Potassium channels
R5-920
Appetite Depressants
medicine
Animals
Obesity
Rats, Wistar
business.industry
Biomedical Sciences
Cell Biology
medicine.disease
Pulmonary hypertension
Acetylcholine
Surgery
lcsh:Biology (General)
chemistry
Calcium Channels
Endothelium, Vascular
Cardiovascular pharmacology
business
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Brazilian Journal of Medical and Biological Research, Volume: 48, Issue: 6, Pages: 537-544, Published: 27 MAR 2015, Brazilian Journal of Medical and Biological Research v.48 n.6 2015, Brazilian Journal of Medical and Biological Research, Associação Brasileira de Divulgação Científica (ABDC), instacron:ABDC, Scopus-Elsevier, Brazilian Journal of Medical and Biological Research, Vol 48, Iss 6, Pp 537-544 (2015)
- Accession number :
- edsair.doi.dedup.....ab859560059087bbeb42fed468a7aabb