Background: Nicotine and nicotinic acetylcholine receptors (nAChRs) have been explored
for the past three decades as targets for pain control. The aim of this review is to introduce
readers particularly to α7 nAChRs in a perspective of pain and its modulation.
Methods: Developments for α7 nAChR modulators and recent animal studies related to pain are
Results: Accumulating evidences suggest that selective ligands for α7 nAChRs hold promise in the
treatment of chronic pain conditions as they lack many of side effects associated with other nicotinic
Conclusion: This review provides the reader recent insights on α7 nAChRs from structure and
function to the latest findings on the pharmacology and therapeutic targeting of these receptors for
the treatment of pain and inflammation.