The best treatment for myocardial infarction is to restore blood flow in the ischaemic region, though it will bring new myocardial damage known as myocardial ischaemia/reperfusion (I/R) injury. Both the ischaemia preconditioning and the ischaemia postcondioning have been shown to reduce the myocardial I/R injury, but their deficits restrict wide clinical availability. It has been demonstrated that inflammation plays a critical role in the I/R injury process. Also plasma levels of cytokines and inflammation response can be regulated by specifically augmenting cholinergic signaling via the efferent vagus nerve and α7 subunit-containing nicotinic acetylcholine receptor (α7nAChR). Because cholinergic modalities, acting through vagus nerve- and/or α7nAChR-mediated mechanism, have been confirmed to suppress excessive inflammation during the I/R injury in kidney, liver, lung and intestine, therefore, we hypothesize that cholinergic agonists may also provide a protection for the myocardial I/R injury.