Figure 1From: Long-acting beta-agonists in the management of chronic obstructive pulmonary disease: current and future agents Indirect and direct relaxation of smooth muscle. Muscarinic antagonists (X) block M3 receptors to prevent binding of acetylcholine (ACh), indirectly stimulating smooth muscle relaxation via inhibition of bronchoconstriction. β2-agonists interact with β2 receptors (β2R) to activate coupling of the stimulatory G protein (Gs) with adenylcyclase (AC). This leads to enhanced production of cyclic adenosine monophosphate (cAMP) which activates protein kinase A (PKA) and results in smooth muscle relaxation. β2-agonists may also interact with presynaptic β2Rs at parasympathetic ganglia, modulating parasympathetic neurotransmission.Back to article page