Document Detail

Receptor pharmacology of carvedilol in the human heart.
MedLine Citation:
PMID:  1378154     Owner:  NLM     Status:  MEDLINE    
The beta-blocker and vasodilator carvedilol was examined in preparations of human ventricular myocardium. Carvedilol is a high-affinity, slightly beta 1-selective competitive beta-blocking agent, with a KD for beta 1-receptors of approximately 4-5 nM and a selectivity of sixfold to 39-fold for beta 1-receptors rather than beta 2-receptors, depending on the method used to assess subtype potency. Carvedilol also is a potent alpha 1-blocking agent, with a beta 1: alpha 1-blocking relative potency of 1.7-fold. In human lymphocytes containing beta 2-receptors and human myocardial membranes containing both beta 1- and beta 2-receptors, carvedilol exhibited the unique property of guanine nucleotide-modulatable binding. This is a property shared with bucindolol, another beta-blocker and vasodilator that is structurally similar to carvedilol. Despite the presence of guanine nucleotide-modulatable binding, no intrinsic activity of carvedilol was detected in preparations of isolated human heart or in myocardial membranes.
M R Bristow; P Larrabee; W Minobe; R Roden; L Skerl; J Klein; D Handwerger; J D Port; B Müller-Beckmann
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of cardiovascular pharmacology     Volume:  19 Suppl 1     ISSN:  0160-2446     ISO Abbreviation:  J. Cardiovasc. Pharmacol.     Publication Date:  1992  
Date Detail:
Created Date:  1992-08-07     Completed Date:  1992-08-07     Revised Date:  2013-05-28    
Medline Journal Info:
Nlm Unique ID:  7902492     Medline TA:  J Cardiovasc Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  S68-80     Citation Subset:  IM    
Cardiology Division, University of Utah Medical Center, Salt Lake City.
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MeSH Terms
Adrenergic beta-Antagonists / metabolism,  pharmacology*
Antihypertensive Agents / metabolism,  pharmacology
Binding, Competitive
Carbazoles / metabolism,  pharmacology*
Cardiomyopathy, Dilated / metabolism*
Cyclic AMP / metabolism
Guanylyl Imidodiphosphate / pharmacology
Metoprolol / metabolism,  pharmacology
Myocardium / metabolism*
Pindolol / analogs & derivatives,  metabolism,  pharmacology
Propanolamines / metabolism,  pharmacology*
Propranolol / metabolism,  pharmacology
Receptors, Adrenergic, beta / drug effects,  metabolism*
Vasodilator Agents / metabolism,  pharmacology*
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 0/Antihypertensive Agents; 0/Carbazoles; 0/Propanolamines; 0/Receptors, Adrenergic, beta; 0/Vasodilator Agents; 0K47UL67F2/carvedilol; 13523-86-9/Pindolol; 34273-04-6/Guanylyl Imidodiphosphate; 37350-58-6/Metoprolol; 525-66-6/Propranolol; 60-92-4/Cyclic AMP; 83498-72-0/Iodocyanopindolol; E9UO06K7CE/bucindolol

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

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