Document Detail


Is the cardiovascular profile of BRL 34915 characteristic of potassium channel activators?
MedLine Citation:
PMID:  2459556     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
To see whether the cardiovascular profile of BRL 34915, a potent vasodilator, is characteristic of potassium channel activators, we investigated its cardiac effects by use of isolated, blood-perfused papillary muscle, sinoatrial (SA) node, and atrioventricular (AV) node preparations of dogs. BRL 34915 was injected intraarterially. It produced an increase in (coronary) blood flow in all preparations. In paced papillary muscle preparations, BRL 34915, although in large doses, produced a decrease in the force of contraction, leading nearly to abolition. The negative inotropic effect of BRL 34915 was accompanied by a marked acceleration of the repolarization of field cardiac action potentials. In some preparations, fibrillation occurred after profound negative inotropy and subsided spontaneously. In unpaced papillary muscles, BRL 34915 in large doses decreased rate of ventricular automaticity. In SA node preparations, BRL 34915 in large doses reduced sinus rate down to approximately 64% of the basal rate and produced atrial standstill in some. In AV node preparations, BRL 34915 in large doses slightly prolonged AV conduction time only when injected into the AV node artery. Nevertheless, it produced third-degree AV block in some. These cardiac effects of BRL 34915 are very similar to those of nicorandil and pinacidil, whose cardiac effects result exclusively from an increase in membrane K conductance in cardiac muscle cells. Like nicorandil and pinacidil, BRL 34915 was highly vasoselective.
Authors:
K Gotanda; K Satoh; N Taira
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of cardiovascular pharmacology     Volume:  12     ISSN:  0160-2446     ISO Abbreviation:  J. Cardiovasc. Pharmacol.     Publication Date:  1988 Aug 
Date Detail:
Created Date:  1988-11-07     Completed Date:  1988-11-07     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7902492     Medline TA:  J Cardiovasc Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  239-46     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Tohoku University School of Medicine, Sendai, Japan.
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MeSH Terms
Descriptor/Qualifier:
Action Potentials / drug effects
Animals
Antihypertensive Agents / pharmacology*
Benzopyrans / pharmacology*
Coronary Circulation / drug effects*
Cromakalim
Dogs
Dose-Response Relationship, Drug
Female
Heart / drug effects*
Heart Conduction System / drug effects
Myocardial Contraction / drug effects
Papillary Muscles / drug effects,  physiology
Potassium Channels / drug effects*
Pyrroles / pharmacology*
Chemical
Reg. No./Substance:
0/Antihypertensive Agents; 0/Benzopyrans; 0/Potassium Channels; 0/Pyrroles; 94470-67-4/Cromakalim

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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