Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors

Ida Nymann Petersen, François Crestey, Anders A Jensen, Dinesh C Indurthi, Henrik Pedersen, Jesper T Andreasen, Thomas Balle, Jesper L Kristensen

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

3 Citationer (Scopus)

Abstract

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.

OriginalsprogEngelsk
TidsskriftA C S Medicinal Chemistry Letters
Vol/bind6
Udgave nummer4
Sider (fra-til)472-475
Antal sider4
ISSN1948-5875
DOI
StatusUdgivet - 9 apr. 2015

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