LAUSR

Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand‐gated ion channels. The α4β2 subtype of nAChRs plays an important role in the mediation of pain and several nicotine‐evoked responses. Agonists and partial agonists of α4β2 nAChRs show efficacy in animal pain models. In addition, the antinociceptive properties of nicotine, a non‐selective nAChR agonist with a high affinity for α4β2 nAChRs, is well‐known. There is a growing body of evidence pointing to allosteric modulation of nAChRs as an alternative treatment strategy in experimental pain. Desformylflustrabromine (dFBr) is a positive allosteric modulator (PAM) at α4β2 nAChRs that enhances agonist responses without activating receptors. We hypothesized that dFBr may enhance nicotine‐induced antinociception.