Document Detail


Pharmacological comparison of the stereoisomers of glyceryl-1-nitrate.
MedLine Citation:
PMID:  8010999     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The enantiomers of glyceryl-1-nitrate, a metabolite of glyceryl trinitrate, were pharmacologically characterized in vitro and in animals. In the Langendorff heart (l) G-1-N was double as potent as (d) G-1-N with respect to the enhancement of coronary flow. The two enantiomers showed almost the same dose-response curves in rabbit aortic strips contracted with phenylephrine. In the same model there were no enantiospecific differences in the development of cross-tolerance to glyceryl-trinitrate. In anaesthetized rabbits, intravenous (l) G-1-N reduced the blood pressure slightly more than (d) G-1-N, while in the conscious dog the blood pressure lowering effect of (d) G-1-N was greater and had a much longer duration (4-6 versus 2 h) than that of (l)G-1-N. The differences in dogs are probably explained by enantiospecific pharmacokinetics: (d) G-1-N had higher plasma levels and showed a longer half-life of elimination than (l) G-1-N (more than 5 h versus 2.7 h). Both enantiomers enhanced the rate of survival after acute coronary ligature in rats with a tendency to higher long-term survival rates after the (d) form.
Authors:
T Zimmermann; M Leitold; H Laufen; K D Riedel; P Stoss
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Publication Detail:
Type:  Comparative Study; In Vitro; Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  44     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1994 Apr 
Date Detail:
Created Date:  1994-07-19     Completed Date:  1994-07-19     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  474-7     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Pfizer/Mack R&D, Illertissen, Fed. Rep. of Germany.
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Animals
Blood Pressure / drug effects
Chinchilla
Coronary Circulation / drug effects
Dogs
Drug Tolerance
Female
Guinea Pigs
Half-Life
Heart / drug effects
Heart Rate / drug effects
Male
Myocardial Contraction / drug effects
Nitroglycerin / analogs & derivatives*,  pharmacokinetics,  pharmacology
Rabbits
Rats
Rats, Sprague-Dawley
Stereoisomerism
Chemical
Reg. No./Substance:
55-63-0/Nitroglycerin; 624-43-1/glycerol-1-nitrate

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


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