Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors
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Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors. / Petersen, Ida Nymann; Crestey, François; Jensen, Anders A; Indurthi, Dinesh C; Pedersen, Henrik; Andreasen, Jesper T; Balle, Thomas; Kristensen, Jesper L.
In: A C S Medicinal Chemistry Letters, Vol. 6, No. 4, 09.04.2015, p. 472-475.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors
AU - Petersen, Ida Nymann
AU - Crestey, François
AU - Jensen, Anders A
AU - Indurthi, Dinesh C
AU - Pedersen, Henrik
AU - Andreasen, Jesper T
AU - Balle, Thomas
AU - Kristensen, Jesper L
PY - 2015/4/9
Y1 - 2015/4/9
N2 - 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.
AB - 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.
U2 - 10.1021/acsmedchemlett.5b00028
DO - 10.1021/acsmedchemlett.5b00028
M3 - Journal article
C2 - 25941557
VL - 6
SP - 472
EP - 475
JO - ACS Medicinal Chemistry Letters
JF - ACS Medicinal Chemistry Letters
SN - 1948-5875
IS - 4
ER -
ID: 140626663