Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors.
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ABSTRACT:
SUBMITTER: Petersen IN
PROVIDER: S-EPMC4416435 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
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Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors.
Petersen Ida Nymann IN Crestey François F Jensen Anders A AA Indurthi Dinesh C DC Pedersen Henrik H Andreasen Jesper T JT Balle Thomas T Kristensen Jesper L JL
ACS medicinal chemistry letters 20150304 4
Conformational restriction of the pyrrolidine nitrogen in nicotine by the introduction of an ethylene bridge provided a potent and selective antagonist of the α4β2-subtype of the nicotinic acetylcholine receptors. Resolution by chiral SFC, pharmacological characterization of the two enantiomers, and determination of absolute configuration via enantioselective synthesis showed that the pharmacological activity resided almost exclusively in the (R)-enantiomer. ...[more]
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