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Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents
Linda P Dwoskin1, Sangeetha P Sumithran, Jun Zhu
1Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA. ldwoskin@uky.edu
Bioorganic & Medicinal Chemistry Letters
|March 31, 2004
Abstract:
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 [(3)H]dopamine release (IC(50)=5 nM; I(max) of 60%), and did not interact with alpha4beta2* or alpha7* nAChRs. bPiDDB represents the current lead compound for development as a tobacco use cessation agent.