Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors

Bioorg Med Chem Lett. 2003 Feb 24;13(4):733-5. doi: 10.1016/s0960-894x(02)01031-4.

Abstract

A total of 20 substituted analogues of nicotine (1a) and homoazanicotine (3a) were examined in order to determine whether or not they might bind in a similar manner at alpha4beta2 nicotinic acetylcholinergic (nACh) receptors. It was found that parallel structural changes in the two series resulted in parallel shifts in affinity. Evidence suggests that the two series are binding in a comparable fashion.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Humans
  • Molecular Mimicry
  • Neurons / chemistry
  • Nicotine / analogs & derivatives*
  • Nicotine / chemical synthesis*
  • Nicotine / chemistry
  • Nicotine / metabolism*
  • Protein Binding
  • Receptors, Nicotinic / metabolism*
  • Structure-Activity Relationship

Substances

  • Receptors, Nicotinic
  • homoazanicotine
  • Nicotine