Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.

Therapeutic Approaches


The discovery and characterization of a novel chemical series of phosphorothioyl-containing imidazopyridines as potent neuropeptide S receptor antagonists is presented. The synthesis of analogues and their structure-activity relationship with respect to the Gq, Gs, and ERK pathways is detailed. The pharmacokinetics and in vivo efficacy of a potent analogue in a food intake rodent model are also included, underscoring its potential therapeutic value for the treatment of sleep, anxiety, and addiction disorders.


Patnaik, Samarjit; Marugan, Juan; Liu, Ke; Zheng, Wei; Southall, Noel; Dehdashti, Seameen J; Thorsell, Annika; Heilig, Markus; Bell, Lauren; Zook, Michelle; Eskay, Bob; Brimacombe, Kyle; Austin, Christopher;


  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Drug Discovery
  • Humans
  • Imidazoles/ chemistry
  • Imidazoles/ pharmacokinetics
  • Imidazoles/ pharmacology
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Neuropeptides/ metabolism
  • Receptors, Neuropeptide/ antagonists & inhibitors
  • Receptors, Neuropeptide/ metabolism
  • Signal Transduction/ drug effects
  • Structure-Activity Relationship

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