Effects of Ranolazine on Vasomotor Responses of Rat Aortic Rings
| Autor: | Ignacio Regla, Dieter Mascher, Ma. Cristina Paredes-Carbajal, Patricia Demare, Ivan Monsalvo, Carlos Hernández-Díaz |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Male
medicine.medical_specialty Endothelium Vasodilator Agents Indomethacin Ranolazine Hemodynamics Vasodilation In Vitro Techniques Nitric Oxide Muscle Smooth Vascular Piperazines Cyclooxygenase pathway Phenylephrine medicine.artery Internal medicine medicine Animals Vasoconstrictor Agents Angina Stable Rats Wistar Aorta Dose-Response Relationship Drug Vasomotor business.industry General Medicine Rats NG-Nitroarginine Methyl Ester medicine.anatomical_structure cardiovascular system Cardiology Acetanilides Endothelium Vascular business medicine.drug |
| Zdroj: | Archives of Medical Research. 44:8-12 |
| ISSN: | 0188-4409 |
| DOI: | 10.1016/j.arcmed.2012.11.002 |
| Popis: | Background and Aims Ranolazine is a piperazine derivative that was approved in 2006 for the treatment of chronic stable angina. Compared with first-line drugs currently used to treat angina, beneficial effects of ranolazine occur without changing hemodynamic parameters such as heart rate and blood pressure. In the present study the effects of ranolazine on vasomotor responses of rat aortic rings were examined. Methods Pharmacological evaluation was performed by analyzing the vasomotor responses of ranolazine on aortic rings of adult male Wistar rats precontracted with phenylephrine (10 −5 M). In each experiment we used a pair of rings (with and without endothelium) from the same aorta and superfused in the same bath. Results Ranolazine (10 −6 –10 −4 M) induced a concentration-dependent relaxation of phenylephrine-precontracted rings. The relaxation was only partially dependent on the presence of the endothelium (56.78 ± 6.81% in rings with endothelium and 47.88 ± 4.70% in rings without endothelium). In rings with endothelium, L-NAME induced a shift to the right of the concentration-response curve to ranolazine. Blocking the cyclooxygenase pathway induced a leftward shift of the concentration relaxation curve to ranolazine in both types of rings and increased the ranolazine-induced relaxation in rings without endothelium. Conclusions Ranolazine has a vasodilatory effect that is predominantly endothelium-independent. The synthesis/release of nitric oxide by the endothelium may, however, contribute to its relaxing action. These effects of ranolazine may contribute to its beneficial effects in patients with stable angina. |
| Databáze: | OpenAIRE |
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