A series of case studies: practical methodology for identifying antinociceptive multi-target drugs

Drug Discov Today. 2012 May;17(9-10):425-34. doi: 10.1016/j.drudis.2012.01.003. Epub 2012 Jan 16.


Since the introduction of drug discovery based on single targets, the number of newly developed drugs has steadily declined, and the reliablility of the current drug-discovery paradigm has been unceasingly questioned. As an alternative, an emerging approach pursuing multi-targeting drugs has arisen to reflect multifactorial diseases caused by the complex networks of various mechanisms. The purpose of this paper is to review multi-target drugs and introduce our progress in establishing a practical methodology for identifying antinociceptive multi-target drugs. We have adopted a system of ex vivo efficacy screening using long-term potentiation in rat spinal cord as a surrogate biomarker for neuropathic pain. A bait-target approach is also adopted to lure an unknown target combination that induces synergistic mechanisms.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Analgesics / pharmacology
  • Analgesics / therapeutic use*
  • Animals
  • Disease Models, Animal*
  • Drug Design
  • Humans
  • Pain / drug therapy*
  • Pain / physiopathology
  • Rats
  • Spinal Cord / drug effects
  • Spinal Cord / physiopathology


  • Analgesics