Lee J, Davis C B, Rivero R A, Reitz A B, Shank R P
R.W. Johnson Pharmaceutical Research Institute, Spring House, Pennsylvania PA 19477, USA.
Bioorg Med Chem Lett. 2000 May 15;10(10):1063-6. doi: 10.1016/s0960-894x(00)00168-2.
The preparation of novel pyridyl ethers as ligands for the nicotinic acetylcholine receptor (nAChR) is described. Variations of the ring size of the azacycle and substitution on the pyridine had dramatic effects on receptor binding affinity with IC50s at the alpha4beta2 nAChR ranging from 22 to >10,000 nM. The most potent molecule was (R)-2-chloro-3-(4-cyanophenyl)-5-((3-pyrrolidinyl)oxy)pyridine 27f with an IC50 of 22 nM.
本文描述了新型吡啶醚作为烟碱型乙酰胆碱受体（nAChR）配体的制备方法。氮杂环环大小的变化以及吡啶上的取代对受体结合亲和力有显著影响，在α4β2 nAChR上的IC50值范围为22至>10,000 nM。最有效的分子是（R）-2-氯-3-（4-氰基苯基）-5-（（3-吡咯烷基）氧基）吡啶27f，IC50为22 nM。
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