Aug 1, 1982

Beta-adrenoceptor-blocking agents: are pharmacologic differences relevant?

American Heart Journal
B J Clark


beta-Adrenoceptor-blocking agents constitute a heterogeneous group of compounds. Membrane- stabilizing (quinidine-like) effects can be demonstrated pharmacologically with most compounds, but only at relatively high concentrations. There is no evidence to suggest that this property is of clinical relevance. Some compounds have a certain selectivity for receptors of the beta 1-type, whereas others possess beta-adrenoceptor stimulant activity (partial agonism). The clinical importance of these latter properties remains controversial. The selectivity for beta 1-adrenoceptors, which can be demonstrated pharmacologically for atenolol, metoprolol, and practolol, appears quite broad. Nevertheless a clear advantage over nonselective compounds with respect to their effects on lung function and vascular resistance in patients has not been established. There are two possible explanations. The first is that the doses used therapeutically may lie outside the selective range; the second is that most tissues appear to possess and mixed population of beta 1- and beta 2-adrenoceptors. According to our present understanding, even absolute specificity for a given subtype cannot provide organ or tissue specificity. Partial agonists provide a consta...Continue Reading

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Mentioned in this Paper

Tissue Specificity
Cardiovascular Diseases
Beta-adrenergic receptor
Norepinephrine Receptors
Sympathomimetic Effect
Plasma Membrane
Adrenergic beta-Antagonists

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