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  • Title: Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents.
    Author: Dwoskin LP, Sumithran SP, Zhu J, Deaciuc AG, Ayers JT, Crooks PA.
    Journal: Bioorg Med Chem Lett; 2004 Apr 19; 14(8):1863-7. PubMed ID: 15050617.
    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.
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