Modulation of neuropeptide Y receptors for the treatment of obesity

Expert Opin Ther Pat. 2009 Oct;19(10):1401-15. doi: 10.1517/13543770903251722.


Background: Neuropeptide Y (NPY) has been demonstrated to have critical roles in the physiological control of appetite and energy homeostasis through NPY Y1, Y2, Y4 and Y5 receptors. A number of synthetic ligands for NPY receptor subtypes have been developed to date, with Y5 receptor antagonists and Y2 and Y4 receptor agonists advancing into clinical trials.

Methods: A survey of the scientific and patent literature since mid-2006 is presented.

Conclusion: In addition to the specific modulation of respective NPY receptor subtypes, recent investigations have revealed that modulation of multiple NPY receptor subtypes produces additive or even synergistic anti-obesity effects. Development of reliable small molecule Y1, Y2 and Y4 receptor ligands would greatly accelerate investigations and drug discovery.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Obesity Agents / chemistry
  • Anti-Obesity Agents / therapeutic use*
  • Drug Design
  • Humans
  • Ligands
  • Molecular Structure
  • Neuropeptide Y / metabolism
  • Obesity / drug therapy*
  • Obesity / metabolism
  • Receptors, Neuropeptide Y / drug effects*
  • Receptors, Neuropeptide Y / metabolism
  • Signal Transduction / drug effects
  • Structure-Activity Relationship
  • Treatment Outcome


  • Anti-Obesity Agents
  • Ligands
  • Neuropeptide Y
  • Receptors, Neuropeptide Y