Abstract
6-(2-Phenylethyl)nicotine (1b; K(i)=15 nM) was unexpectedly found to bind at alpha4beta2 nicotinic cholinergic (nACh) receptors. Although this compound failed to produce nicotine-like agonist action in several functional assays, 1b antagonized the antinociceptive effects of nicotine (mouse tail-flick assay) in a dose-dependent fashion when administered via an intrathecal route.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Analgesics / antagonists & inhibitors
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Animals
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Cholinergic Agents / chemical synthesis*
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Cholinergic Agents / pharmacology
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Ligands
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Male
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Mice
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Mice, Inbred ICR
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Nicotine / analogs & derivatives*
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Nicotine / chemical synthesis
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Nicotine / pharmacology
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Receptors, Nicotinic / drug effects*
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Structure-Activity Relationship
Substances
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6-(2-phenylethyl)nicotine
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Analgesics
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Cholinergic Agents
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Ligands
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Receptors, Nicotinic
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nicotinic receptor alpha4beta2
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Nicotine