Document Detail


Cardiac electrophysiologic actions of SCH 19927 (Dilevalol), the R,R-isomer of labetalol.
MedLine Citation:
PMID:  3795037     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The cardiac electrophysiologic, hypotensive and antiadrenergic actions of SCH 19927, the R,R-isomer of labetalol, were evaluated in urethane-anesthetized dogs. The cumulative administration of 0.3, 1.0 and 3.0 mg/kg i.v. decreased mean arterial pressure by 18 to 26 mm Hg from a pretreatment value of 106 +/- 6 mm Hg and slightly enhanced atrioventricular nodal conduction. After 3.0 mg/kg of SCH 19927, sinoatrial (SA) conduction times were decreased, whereas intraventricular conduction was depressed slightly. SCH 19927, 10.0 mg/kg, reduced mean arterial pressure by 39 mm Hg and enhanced SA nodal conduction and recovery after overdrive pacing (decreased SA conduction time and corrected sinus node recovery times), whereas intraventricular conduction times and the rate-corrected QTc interval were prolonged. Sinus heart rate, atrial, ventricular and atrioventricular nodal functional and effective refractory periods were unaltered by SCH 19927, 0.3 to 10.0 mg/kg. The administration of SCH 19927 produced significant beta adrenergic receptor blockade, as determined by inhibition of the positive chronotropic and peripheral vasodilatory response to isoproterenol, but did not alter the alpha-1 adrenergic receptor-mediated vasopressor response to phenylephrine. The results indicate that SCH 19927, in beta adrenergic receptor blocking and hypotensive dosages, does not depress SA nodal or atrioventricular nodal function, thus suggesting an electrophysiologic spectrum of activity different from that of other beta adrenergic receptor antagonists.
Authors:
J J Lynch; D G Montgomery; B R Lucchesi
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  The Journal of pharmacology and experimental therapeutics     Volume:  239     ISSN:  0022-3565     ISO Abbreviation:  J. Pharmacol. Exp. Ther.     Publication Date:  1986 Dec 
Date Detail:
Created Date:  1987-01-30     Completed Date:  1987-01-30     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0376362     Medline TA:  J Pharmacol Exp Ther     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  719-23     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Atrioventricular Node / drug effects
Blood Pressure / drug effects
Dogs
Electrophysiology
Heart / drug effects*
Heart Rate / drug effects
Isomerism
Isoproterenol / pharmacology
Labetalol / pharmacology*
Male
Grant Support
ID/Acronym/Agency:
HL-05806-26/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
36894-69-6/Labetalol; 7683-59-2/Isoproterenol

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


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