Characterization of β1‐selectivity, adrenoceptor‐Gs‐protein interaction and inverse agonism of nebivolol in human myocardium
Key result
Nebivolol demonstrated 3-4 fold beta1-selectivity compared to 16-20 fold for bisoprolol in human myocardium, with similar inverse agonist activity, suggesting other mechanisms drive its clinical effects.
Authors
Discussion
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Implication
Questions nebivolol's beta1-selectivity advantage versus bisoprolol; leaves open alternative mechanisms for its clinical effects.
PICO
P
Population
Failing and nonfailing myocardium
I
Intervention / Comparator
Nebivolol vs Bisoprolol, bucindolol, carvedilol, and metoprolol
O
Primary Outcome
Beta1-selectivity and intrinsic activity
Cite This Study
Maack et al. (2001) studied Failing and nonfailing myocardium. Nebivolol vs. Bisoprolol, bucindolol, carvedilol, and metoprolol was evaluated on Beta1-selectivity and intrinsic activity. Nebivolol demonstrated 3-4 fold beta1-selectivity compared to 16-20 fold for bisoprolol in human myocardium, with similar inverse agonist activity, suggesting other mechanisms drive its clinical effects.