Dimensions of the ion channel in neuronal nicotinic acetylcholine receptor as estimated from analysis of conformation-activity relationships of open-channel blocking drugs Journal Articles uri icon

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  • Relationship between the size of the molecule in the series of organic ions Et3+N--(CH2)5--+NR1R2R3 (Ri--alkyl or cycloalkyl substituents) and their abilities to block nicotinic acetylcholine receptors (AChRs) due to their open-channel blockade in the neurons of autonomic ganglia and in frog end-plate was analyzed. All low-energy equilibrium conformations of the drugs were calculated by the molecular mechanics method. A unique rectangular channel profile 6.1 x 8.3 A, for which the best correlation between blocking activity of the drugs and total population of their conformations being able to penetrate into the channel, was deduced from all those tested.


  • Zhorov, Boris
  • Brovtsyna, Nina B
  • Gmiro, Valeriy E
  • Lukomskaya, Nera Ya
  • Serdyuk, Sergei E
  • Potapyeva, Natalva N
  • Magazanik, Lev G
  • Kurenniy, Dmitriy E
  • Skok, Vladimir I

publication date

  • April 1991