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M. B. Fowler, Cardiac adrenoceptors in the failing heart: effect of intervention, European Heart Journal, Volume 11, Issue suppl_A, April 1990, Pages 13–18, https://doi.org/10.1093/eurheartj/11.suppl_A.13
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Abstract
The sympathetic nervous system is chronically activated in heart failure. This results in a reduction in numbers and sensitivity of β-receptors, making the heart less responsive to the actions of catecholamines. This is specific to β-receptors, the adenycyclase system being largely unaffected.
Sympathomimetic agents are still used in patients with heart failure to augment cardiac contractility, but tachyphylaxis limits their long-term usefulness, and they may actually cause further myocardial damage. On the other hand, β-blockade can improve sensitivity to catecholamines and cardiac action in some patients with severe left ventricular dysfunction, although this treatment can be hazardous and cannot yet be routinely recommended.
Partial β-agonists are theoretically useful since they can provide bareline sympathetic drive while protecting the heart against excessive sympathetic stimulation and down-regulation of β-receptors. Xamoterol, a partial agonist with half the sympathetic activity of isoprenaline, has been shown to be superior to placebo and to digoxin in patients with mild to moderate heart failure.