Document Detail

Effects of beta-adrenoreceptor blocking drugs on adrenergic transmission.
MedLine Citation:
PMID:  6246     Owner:  NLM     Status:  MEDLINE    
The peripheral actions of beta-adrenoreceptor antagonists on adrenergic transmitter mechanisms have been reviewed. In addition to receptor blockade, beta-adrenoreceptor antagonists may in high concentrations inhibit neuronal uptake of noradrenaline; inhibit monoamine oxidase; inhibit the uptake of noradrenaline into transmitter storage vesicles and inhibit the extraneuronal uptake of noradrenaline. High concentrations of beta-adrenoreceptor antagonists (threshold about 30 muM) also release noradrenaline from intraneuronal stores; however, their intrinsic sympathomimetic activity is generally attributed to their partial agonist property. Beta-adrenoreceptor antagonists possess adrenergic neurone blocking activity and quinidine-like or local anaesthetic activity. The existance of a positive feedback mechanism involving prejunctional beta-adrenoreceptors is discussed. It is suggested that bradycardia produced by beta-adrenoreceptor antagonists is due to blockade of the action of circulating catecholamines or of transmitter noradrenaline at cardiac extrajunctional beta-adrenoreceptor sites.
M Rand; M Law; D F Story; M W McCulloch
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Drugs     Volume:  11 SUPPL 1     ISSN:  0012-6667     ISO Abbreviation:  Drugs     Publication Date:  1976  
Date Detail:
Created Date:  1976-09-01     Completed Date:  1976-09-01     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7600076     Medline TA:  Drugs     Country:  SWITZERLAND    
Other Details:
Languages:  eng     Pagination:  134-43     Citation Subset:  IM    
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MeSH Terms
Adrenergic beta-Antagonists / pharmacology*
Depression, Chemical
Electric Stimulation
Guinea Pigs
Monoamine Oxidase Inhibitors / pharmacology
Neuromuscular Junction / drug effects
Neurons / drug effects,  metabolism
Neurotransmitter Agents / metabolism
Norepinephrine / metabolism
Receptors, Adrenergic / drug effects
Sympathetic Nervous System / physiology*
Sympathomimetics / pharmacology
Synaptic Transmission / drug effects*
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 0/Monoamine Oxidase Inhibitors; 0/Neurotransmitter Agents; 0/Receptors, Adrenergic; 0/Sympathomimetics; 51-41-2/Norepinephrine

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

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