Document Detail


Centrally induced cardiovascular effects and kinetic behaviour of isoarecaidine propyl ester in the cat.
MedLine Citation:
PMID:  7092417     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The present investigation deals with effects of isoarecaidine propyl ester (IAPE) on blood pressure and heart rate of the anaesthetized cat. The kinetic behaviour of the drug in plasma and various brain tissues was also studied. The results indicate that the ester (4 mg.kg-1) induces a depressor effect and bradycardia after i.v. administration. Injection of IAPE (up to 60 micrograms.kg-1) into the left vertebral artery lowers blood pressure in a dose-dependent manner. When administered simultaneously into the left and right vertebral artery, low doses (6 micrograms. kg-1) produce a substantial fall in blood pressure. Although the fall in blood pressure after i.v. injection lasts for more than 60 min, plasma half life is extremely short (t1/2 = 6.3 sec). The possible metabolism of the ester was studied in the pons, medulla oblongata and cerebellum. Thirty min after the injection into the left vertebral artery, IAPE is almost entirely hydrolyzed in the pontomedullary region. This degradation is prevented by pretreatment with paraoxon, that abolishes the depressor action of IAPE. It is suggested that accumulated isoarecaidine in the pontomedullary region is responsible for the depressor response to IAPE. Since IAPE does not seem to influence blood pressure and heart rate via a peripheral mechanism and lowers blood pressure and cardiac frequency by a central action, this drug is considered to be of pharmacological interest. The mechanism of action is discussed.
Authors:
A J Porsius; G Lambrecht; U Moser; E Mutschler
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Archives internationales de pharmacodynamie et de thérapie     Volume:  256     ISSN:  0003-9780     ISO Abbreviation:  Arch Int Pharmacodyn Ther     Publication Date:  1982 Mar 
Date Detail:
Created Date:  1982-08-26     Completed Date:  1982-08-26     Revised Date:  2012-01-12    
Medline Journal Info:
Nlm Unique ID:  0405353     Medline TA:  Arch Int Pharmacodyn Ther     Country:  BELGIUM    
Other Details:
Languages:  eng     Pagination:  22-35     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Blood Pressure / drug effects*
Brain / drug effects*,  metabolism
Cardiovascular Agents / metabolism,  pharmacology*
Cats
Female
Isonicotinic Acids / metabolism,  pharmacology*
Kinetics
Male
Chemical
Reg. No./Substance:
0/Cardiovascular Agents; 0/Isonicotinic Acids; 77035-54-2/isoarecaidine propyl ester

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


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