Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3157-60. doi: 10.1016/s0960-894x(02)00652-2.

Abstract

A series of aminoalkylazetidines has been discovered as novel ORL1 receptor ligands. Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified.

MeSH terms

  • Animals
  • Azetidines / chemical synthesis*
  • Azetidines / pharmacology*
  • Binding, Competitive / drug effects
  • CHO Cells
  • Cricetinae
  • Diprenorphine / pharmacology
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Humans
  • Indicators and Reagents
  • Ligands
  • Narcotic Antagonists / pharmacology
  • Nociceptin
  • Nociceptin Receptor
  • Opioid Peptides / metabolism
  • Receptors, Opioid / drug effects*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Azetidines
  • Indicators and Reagents
  • Ligands
  • Narcotic Antagonists
  • Opioid Peptides
  • Receptors, Opioid
  • Diprenorphine
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Nociceptin Receptor