The cholinergic anti-inflammatory pathway (CAP) is a new neurophysiologic mechanism regulating the immune system, with alpha7 nicotinic acetylcholine receptor (α7nAChR) being its potential pharmacological target. Cumulative studies have demonstrated that activation of α7nAChR can inhibit inflammation through modulating pro-inflammatory cytokines. The role of α7nAChR has been confirmed in a series of inflammatory diseases. This review is aimed to provide new insights for using α7nAChR against inflammatory diseases.