Chronic pain represents a prevalent and costly medical challenge globally. Nicotinic acetylcholine
receptors (nAChRs), one type of ligand-gated ion channels found extensively in both the central
and peripheral nervous systems, have emerged as promising therapeutic targets for chronic pain.
Although there are currently no FDA-approved analgesics specifically targeting nAChRs, accumulating
preclinical and clinical evidence suggest that selective ligands for alpha 7 (α7) nAChRs show potential
for treating chronic pain, boasting a reduced incidence of side effects compared with other nicotinic
receptor types. The recent structural resolution of human α7 nAChRs has confirmed their negative
association with heightened pain, providing a valuable foundation for the development of targeted
medications. This review presents a comprehensive overview, encompassing insights into the roles of
α7 nAChRs derived from structural and functional studies, recent advancements in pharmacology, and
investigations into their involvement in the pathophysiology of chronic pain. Moreover, the review
addresses the variability in analgesic effects based on the type of receptor agonist and highlights the
current research limitations. As such, this review offers potential therapeutic approaches for the development
of innovative strategies for chronic pain management.