Synthesis and binding of 3-aminopyridine derivatives at central nicotinic receptors

Arzneimittelforschung. 2000 Jun;50(6):507-11. doi: 10.1055/s-0031-1300238.

Abstract

A series of secondary and tertiary pyridyl amides as potential central nicotinic acetylcholine receptors (nAChRs) ligands were prepared. Amides displayed negligible or very low affinity, whereas two amines achieved by reduction of corresponding secondary amides, showed affinity in the nanomolar range for nAChRs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminopyridines / chemical synthesis*
  • Aminopyridines / metabolism*
  • Animals
  • Central Nervous System / drug effects
  • Central Nervous System / metabolism*
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • Chemical Phenomena
  • Chemistry, Physical
  • In Vitro Techniques
  • Male
  • Nicotine / metabolism
  • Nicotinic Agonists / metabolism
  • Rats
  • Rats, Wistar
  • Receptors, Nicotinic / drug effects
  • Receptors, Nicotinic / metabolism*
  • Structure-Activity Relationship

Substances

  • Aminopyridines
  • Nicotinic Agonists
  • Receptors, Nicotinic
  • Nicotine