Document Detail


Blockade of putative beta4- and beta1-adrenoceptors by carvedilol in ferret myocardium.
MedLine Citation:
PMID:  10498290     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The putative beta4-adrenoceptor mediates positive inotropic effects, action potential shortening and arrhythmias in ferret ventricle. Here we compared the affinity of carvedilol at the putative beta4-adrenoceptor and beta1-adrenoceptor, activated by (+/-)-CGP 12177 and (-)-isoprenaline, respectively. In paced right ventricular preparations, carvedilol (0.01-10 micromol/l) was a simple competitive antagonist of the positive inotropic effects of (+/-)-CGP 12177 (slope of Schild-plot = 1.02, pK(B) = 6.8) and (-)-isoprenaline (slope of Schild-plot = 0.98, pK(B) = 8.1). Carvedilol also blocked putative beta4- and beta1-adrenoceptors of left ventricle, left atrium and sino-atrial pacemaker. Carvedilol therefore interacts with the putative beta4-adrenoceptor according to the law of mass action and may provide a lead in the development of putative beta4-adrenoceptor-selective antagonists.
Authors:
M D Lowe; A A Grace; A J Kaumann
Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Naunyn-Schmiedeberg's archives of pharmacology     Volume:  359     ISSN:  0028-1298     ISO Abbreviation:  Naunyn Schmiedebergs Arch. Pharmacol.     Publication Date:  1999 May 
Date Detail:
Created Date:  1999-09-28     Completed Date:  1999-09-28     Revised Date:  2013-05-28    
Medline Journal Info:
Nlm Unique ID:  0326264     Medline TA:  Naunyn Schmiedebergs Arch Pharmacol     Country:  GERMANY    
Other Details:
Languages:  eng     Pagination:  400-3     Citation Subset:  IM    
Affiliation:
Department of Biochemistry, University of Cambridge, UK.
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MeSH Terms
Descriptor/Qualifier:
Adrenergic beta-Agonists / pharmacology
Adrenergic beta-Antagonists / pharmacology*
Animals
Carbazoles / pharmacology*
Dose-Response Relationship, Drug
Ferrets*
Heart Atria / drug effects
Heart Ventricles / drug effects
Isoproterenol / pharmacology
Male
Myocardial Contraction
Myocardium / metabolism*
Propanolamines / pharmacology*
Receptors, Adrenergic, beta / drug effects*
Sinoatrial Node / drug effects
Chemical
Reg. No./Substance:
0/Adrenergic beta-Agonists; 0/Adrenergic beta-Antagonists; 0/Carbazoles; 0/Propanolamines; 0/Receptors, Adrenergic, beta; 0/adrenergic beta-4 receptor; 0K47UL67F2/carvedilol; 7683-59-2/Isoproterenol; 81047-99-6/CGP 12177

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


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