Effect of a novel stobadine derivative on isolated rat arteries
| Autor: | Ruzena Sotnikova, Zuzana Broskova, Zsolt Bagi, Jana Nedelcevova |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
medicine.medical_specialty
Contraction (grammar) Health Toxicology and Mutagenesis Potassium arterioles chemistry.chemical_element Pharmacology Toxicology Contractility medicine.artery medicine Phenylephrine pyridoindole Aorta Vasomotor business.industry SMe1EC2 Surgery aorta chemistry Original Article Serotonin business Ex vivo medicine.drug |
| Zdroj: | Interdisciplinary Toxicology |
| ISSN: | 1337-9569 1337-6853 |
| DOI: | 10.2478/intox-2013-0011 |
| Popis: | The antioxidant and reactive-oxygen-species-scavenging activity of stobadine has been demonstrated in previous studies. Recently, chemical modification of this leading structure led to the synthesis of other pyridoindole derivatives with significantly increased intrinsic antioxidant efficacy. Further structural modifications of stobadine provided the opportunity to increase bioavailability and attenuate unwanted side effects, such as α-adrenolytic activity. The aim of the work was to evaluate the direct effect of a novel pyridoindole, SMe1EC2, on the vascular wall ex vivo. The vasomotor effect of SMe1EC2 (1×10-8-1×10-4 mol/l) was measured on isolated and pressurized rat cerebral and coronary arterioles using video-microscopy. The effect of SMe1EC2 (1×10-6 and 1×10-5 mol/l) on high potassium-, phenylephrine- or serotonin-induced contraction or acetylcholine-induced relaxation was also determined in aortic rings. We found that SMe1EC2 (1×10-8-1×10-4 mol/l) elicited significant dilatations in both cerebral and coronary arterioles (max dilatation: 25±8% and 18±5% respectively). Yet, SMe1EC2 (1×10-6 and 1×10-5 mol/l) did not influence the tone of aortic rings nor did it affect high potassium-, phenylephrine- or serotonin -induced contractions and acetylcholine-induced relaxation. Thus SMe1EC2 was able to dilate resistance arteries but did not affect aortic contractility. It is likely that SMe1EC2 does not possess α1-adrenolytic and anti-serotoninergic activity in the vascular wall. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|