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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Biological Assay
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Male
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Molecular Structure
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Nicotine / pharmacology
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Nicotinic Antagonists / chemistry
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Nicotinic Antagonists / pharmacology*
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Picolines / chemistry
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Picolines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Nicotinic / drug effects*
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Receptors, Nicotinic / metabolism
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Smoking Cessation*
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Structure-Activity Relationship
Substances
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Nicotinic Antagonists
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Picolines
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Receptors, Nicotinic
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Nicotine