Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.

@article{Wei2005NovelPR,
  title={Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.},
  author={Zhi-Liang Wei and Yingxian Xiao and Hongbin Yuan and Maryna Baydyuk and Pavel A. Petukhov and John L. Musachio and Kenneth Jon Kellar and Alan P. Kozikowski},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 6},
  pages={
          1721-4
        }
}
Introduction of a hydrophobic or hydrogen-bonding alkynyl group into the C5 position of the pyridyl ring of epibatidine and A-84543 significantly increased the selectivity for neuronal nicotinic acetylcholine receptors (nAChRs) containing beta2 subunits over nAChRs containing beta4 subunits (K(i) ratio up to 92000-fold). Our data indicate that the extracellular domains of the nAChRs are sufficiently different to allow for the design of novel ligands with high affinity and selectivity for the… CONTINUE READING
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