Although the disease-modifying anti-rheumatic drugs (DMARD) have been widely used in clinics, rheumatoid arthritis (RA) is not completely curable so far. Hence, to seek new drugs for the treatment of RA has become a pursuing goal of rheumatologists and orthopedic surgeons. Since the major pathological characteristic of RA is inflammation, the exploration of anti-inflammatory drugs has become a hotspot. Moreover, the anti-inflammatory and anti-nociceptive functions of nicotinic acetylcholine receptors as well as the related mechanisms have been recently discovered. Based on the above-mentioned, it is promising that the nicotinic acetylcholine receptor agonists will be applied for the treatment of RA. Following in vitro, in vivo experiments as well as clinical trials will even strengthen this viewpoint and more RA patients will benefit from the application of such agents.