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Comment
. 2009 Feb 17;106(7):2095-6.
doi: 10.1073/pnas.0812935106. Epub 2009 Feb 11.

Agonizing over agonism: should asthmatics turn their beta-receptors on or off?

Raymond B Penn  1
Affiliations
Comment

Agonizing over agonism: should asthmatics turn their beta-receptors on or off?

Raymond B Penn. Proc Natl Acad Sci U S A. .
No abstract available

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Conflict of interest statement

The author declares no conflict of interest.

Figures

Fig. 1.
Fig. 1.
β2AR agonism in the asthmatic airway, a potential model suggested by findings of Nguyen et al. (4). β2AR activation (“β2AR on”), resulting from constitutive β2AR activity, endogenous catecholamines, or inhaled β-agonists, has a permissive effect on airway inflammation that generates contractile agents causing airway smooth muscle (ASM) contraction and promotes airway mucus secretion that increases airway resistance. Direct effects of β-agonists on ASM antagonize effects of contractile agents to prevent/reverse bronchoconstriction. Airflow conductance is affected by the competitive actions of procontractile and prorelaxant effects on ASM, and by impedance caused by airway mucus. Alternatively, β2AR inverse agonists (“β2AR off”) inhibit all β2AR activity, resulting in inhibition of allergic inflammation and null or modest inhibition the bronchoprotective/relaxing effect of β2AR activity in ASM. ASM contractile state and airflow are effectively managed by the anti-inflammatory effects that reduce levels of bronchoactive agents and mucus.
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