Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5275-9. doi: 10.1016/j.bmcl.2004.08.032.


Small molecule mu agonists based on the 4-phenyl piperidine scaffold were designed and synthesized to further investigate the therapeutic potential of loperamide analogs. The resulting compounds show excellent agonistic activity towards the human mu receptor with interesting SAR trends within the series.

MeSH terms

  • Cell Line
  • Humans
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology*
  • Receptors, Opioid, mu / agonists*
  • Receptors, Opioid, mu / antagonists & inhibitors
  • Receptors, Opioid, mu / metabolism
  • Structure-Activity Relationship


  • Piperidines
  • Receptors, Opioid, mu