Nebentan - CAS 403604-85-3
Catalog number:
403604-85-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
Nebentan, also known as YM598, is an orally active synthetic substituted phenylethenesulfonamide. As a selective endothelin A receptor antagonist, YM598 inhibits endothelin-mediated mechanisms involved in tumor cell growth and progression, angiogenesis, and metastasis.
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Synonyms:
YM598; YM 598; YM-598
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Current Developer:
Astellas Pharma Inc
1.[Comparison of the efficacy and safety of electrical cardioversion and pharmacological cardioversion with nibentan in patients with persisting atrial fibrillation and flutter].
Giliarov MIu, Novikova NA, Sulimov VA, Suchkova SA, Syrkin AL. Vestn Ross Akad Med Nauk. 2007;(5):22-6.
The aim of the study was to compare the efficacy and safety of pharmacological cardioversion (PC) by nibentan, a class III antiarrhythmic agent, and electrical cardioversion (EC) in patients with persisting atrial fibrillation (AFib) and atrial flutter (AFI) receiving basic antiarrhythmic therapy. Ninety-seven patients with persisting AFib and AFI were included in the trial (45 patients constituted PC group, and 52 constituted EC group). Both groups were comparable according to basic demographic and clinical parameters as well as antiarrhythmic therapy being applied. The results of the study showed that the efficacy of PC did not differ from that of EC (86.7% and 92.3% respectively, p = 0.282). the frequency of arrhythmogenic effect did not differ between the groups either (p = 0.46). One case of non-stable ventricular tachycardia was registered in the PC group. The most significant adverse effect was bradicardia, which was registered more often in the PC group than in EC group (26.
2.Myocardial contractility after in vitro treatment with class III antiarrhythmic drug Nibentan.
Latfullin IA1, Gaifullina RF, Dzhordzhikiya RK, Nigmatullina RR. Bull Exp Biol Med. 2006 Jan;141(1):81-3.
Myocardial contractility was studied in vitro in response to treatment with class III antiarrhythmic drug Nibentan. The contractile response to Nibentan in increasing concentrations of 1.66, 2.5, and 3.5 mM was estimated on strips of animal myocardium and human right atrial auricle.
3.[Effect of nibentan on dispersion of repolarization of ventricular myocardium in the rabbit].
Glukhov AV, Reznik AV, Kovalenko NV, Egorov IuV, Rozenshtraukh LV. Kardiologiia. 2008;48(7):40-7.
Among factors determining development of polymorphic ventricular tachycardia torsades de pointes under influence of class III antiarrhythmic drugs great value is attributed to enhanced heterogeneity of repolarization of ventricular myocardium which can cause functional conduction blocks and development of re-entry of excitation. In this work with the help of optical mapping of electrical activity of the heart we investigated effect of nibentan (0.3 and 1 mM) on chronotopography of repolarization of epicardial surface of ventricles of isolated after Langendorf rabbit heart (n=5). For assessment of heterogeneity of repolarization we measured the following parameters: standard deviation of mean action potential duration (APDm) along mapped region (SD-APD), dispersion index (DI=1000 SD-APDm), maximal dispersion (Dmax=APDmax-APDmin). Nibentan in concentrations 0.3 and 1 mM increased APD at the level of 90% repolarization (APD90%) from 231 +/- 12 to 277 +/- 7 ms (p < 0.
4.[The efficacy and safety of nibentan for pharmacological cardioversion in patients with persistent atrial fibrillation and flutter: the role of dose limitation and magnesium sulfate administration].
Bregvadze IN, Maĭkov EB, Bil'dinov OA, Kratskina TL, Klimenko IuL, Smirnova MIu, Sokolov SF, Golitsyn SP, Rozenshtraukh LV, Chazov EI. Kardiologiia. 2007;47(3):48-55.
The aim of the study was to evaluate the influence of magnesium sulfate on the efficacy and safety of pharmacological cardioversion with nibentan (NB) in doses up to 0,125 mg/kg in patients with persistent atrial fibrillation (AF) and flutter (AFL). Calculated dose of NB was 0.125 mg/kg. It was administered as 2 bolus injections (0.0625 mg/kg each) performed with the interval of 15 minutes. The study included 64 patients (pts) (45 male, age 54+/-9,9 years) with persistent AF (n=56) and AFL (n=8) with median arrhythmia duration 6,7+/-6,8 months (8 days to 36 months). Pts were divided into two groups. In the first (I) group NB was used without preliminary magnesium sulfate administration, in the second group (II) magnesium sulfate was injected in a dose of 50 mg/kg, followed by 0.83 mg/kg/min infusion before NB administration. There was no difference between groups in conversion rates of atrial arrhythmias: 74% and 69%, in groups I and II, respectively (p>0.
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CAS 403604-85-3 Nebentan

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