A comparison of the binding of three series of nicotinic ligands

Bioorg Med Chem Lett. 2002 Aug 5;12(15):1989-92. doi: 10.1016/s0960-894x(02)00298-6.

Abstract

A total of 24 aryl-substituted analogues of nicotine (1a) and two related series of nicotinic ligands, aminomethylpyridines 3 and ether analogues 8, were examined to determine if they bind at alpha4beta2 nACh receptors in a common manner. A modest correlation (r=0.785) was found between the affinities of the nicotine analogues and derivatives of 3, but little correlation (r=0.348) was found with analogues 8. However, a modest correlation (r=0.742) exists between the binding of analogues 3 and 8. It seems that 1-series and 8-series compounds bind differently but that the 3-series compounds share some intermediate binding similarity with both.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Brain / metabolism
  • Chemical Phenomena
  • Chemistry, Physical
  • Ether / analogs & derivatives
  • Isoquinolines / chemistry
  • Kinetics
  • Ligands
  • Nicotine / analogs & derivatives*
  • Nicotine / metabolism*
  • Protein Binding
  • Pyridines / chemistry
  • Radioligand Assay
  • Rats
  • Receptors, Nicotinic / metabolism*
  • Statistics as Topic
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Isoquinolines
  • Ligands
  • Pyridines
  • Receptors, Nicotinic
  • nicotinic receptor alpha4beta2
  • Ether
  • Nicotine