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.
G Ferretti  1 ,  M Dukat ,  M Giannella ,  A Piergentili ,  M Pigini ,  W Quaglia ,  M I Damaj ,  B R Martin ,  R A Glennon
Affiliations
  • 1. Department of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23298, USA.
PMID: 12639569 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.

Products