| Title : Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors - Petersen_2015_ACS.Med.Chem.Lett_6_472 |
| Author(s) : Petersen IN , Crestey F , Jensen AA , Indurthi DC , Pedersen H , Andreasen JT , Balle T , Kristensen JL |
| Ref : ACS Med Chem Lett , 6 :472 , 2015 |
|
Abstract :
Conformational restriction of the pyrrolidine nitrogen in nicotine by the introduction of an ethylene bridge provided a potent and selective antagonist of the alpha4beta2-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. |
| PubMedSearch : Petersen_2015_ACS.Med.Chem.Lett_6_472 |
| PubMedID: 25941557 |
Petersen IN, Crestey F, Jensen AA, Indurthi DC, Pedersen H, Andreasen JT, Balle T, Kristensen JL (2015)
Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors
ACS Med Chem Lett
6 :472
Petersen IN, Crestey F, Jensen AA, Indurthi DC, Pedersen H, Andreasen JT, Balle T, Kristensen JL (2015)
ACS Med Chem Lett
6 :472