Abstract:
:N-[3,5-Dichlorophenyl] 4-[4-hydroxy-2-methoxy-phenyl] piperazine carboxamidine dihydrochloride (RS-87337) is a chemically novel antiarrhythmic agent with an electrophysiologic profile characteristic of both class III and class Ia compounds as defined by Vaughan-Williams and Campbell. In isolated superfused guinea pig papillary muscles, RS-87337 (0.1-10 microM) prolonged the duration of the action potential (class III effect) and at higher concentrations (10-30 microM) reduced the maximum rate of membrane depolarisation (class I effect). The rate of onset and of recovery from the latter activity was similar to that of disopyramide, between that of lignocaine and flecainide, which allowed its placement in subclass Ia. When perfused into isolated working rat hearts, RS-87337 (10-1,000 nM) reduced the incidence of ventricular fibrillation that followed coronary artery reperfusion and in anaesthetised rats [RS-87337, 1-5 mg/kg intravenously (i.v.)] enabled more animals to survive the tachycardia, fibrillation, and mortality produced by a similar procedure. In conscious dogs, i.v. (3-10 mg/kg) and oral (15-60 mg/kg) doses of RS-87337 reduced the number of the ectopic electrocardiogram (ECG) complexes observed 24 h after a two-stage coronary ligation. In anaesthetised dogs with paced hearts, i.v. doses of RS-87337 (0.02-5.0 mg/kg) reduced the elevated ECG S-T segment evoked by brief coronary artery occlusion without altering baseline haemodynamic values. We assume that the class III and Ia effects of RS-87337 made an important contribution to the compound's antiarrhythmic and cardioprotective effects.
journal_name
J Cardiovasc Pharmacoljournal_title
Journal of cardiovascular pharmacologyauthors
Dumez D,Patmore L,Ferrandon P,Allely M,Armstrong JMdoi
10.1097/00005344-198908000-00002subject
Has Abstractpub_date
1989-08-01 00:00:00pages
184-93issue
2eissn
0160-2446issn
1533-4023journal_volume
14pub_type
杂志文章abstract::The electrophysiologic effects of the metabolites of verapamil are unknown and may contribute to the observed differences between intravenous and oral verapamil. We examined the electrophysiologic effects of verapamil and its metabolites (norverapamil, N-dealkylverapamil (D617), and N-dealkylnorverapamil (D620)) at es...
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章
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更新日期:2000-07-01 00:00:00
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pub_type: 杂志文章
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journal_title:Journal of cardiovascular pharmacology
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journal_title:Journal of cardiovascular pharmacology
pub_type: 杂志文章,评审
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journal_title:Journal of cardiovascular pharmacology
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journal_title:Journal of cardiovascular pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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