Subtype-selective nicotinic receptor antagonists: Potential as tobacco use cessation agents

Article abstract of DOI:10.1016/j.bmcl.2003.10.073

N-n-Alkylpicolinium and N,N′-alkyl-bis-picolinium analogues were assessed in nicotinic receptor (nAChR) assays. The most potent and subtype-selective analogue, N,N′-dodecyl-bis-picolinium bromide (bPiDDB), inhibited nAChRs mediating nicotine-evoked [³H]dopamine release (IC₅₀=5 nM; I_max of 60%), and did not interact with α4β2* or α7* nAChRs. bPiDDB represents the current lead compound for development as a tobacco use cessation agent.