Mechanism of action
Activation of β adrenergic receptors leads to relaxation of smooth muscle in the lung, and dilation and opening of the airways.
β adrenergic receptors are coupled to a stimulatory G protein of
adenylyl cyclase. This enzyme produces the second messenger
cyclic adenosine monophosphate (cAMP). In the lung, cAMP decreases calcium concentrations within cells and activates
protein kinase A. Both of these changes, inactivate
myosin light-chain kinase and activate
myosin light-chain phosphatase. In addition, β2 agonists open large conductance
calcium-activated potassium channels and thereby tend to hyperpolarize airway smooth muscle cells. The combination of decreased intracellular calcium, increased membrane potassium conductance, and decreased myosin light chain kinase activity leads to smooth muscle relaxation and bronchodilation.