Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4389-93. doi: 10.1016/j.bmcl.2003.09.024.

Abstract

A novel non-vanilloid VR1 antagonist consisting of a new vanilloid equivalent exhibits excellent analgesic effects as well as highly potent antagonistic activities in both capsaicin single channel and calcium uptake assays. In addition, the structural requirement for the vanilloid equivalent of the potent VR1 antagonist has also been elucidated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemical synthesis*
  • Analgesics / chemistry
  • Analgesics / pharmacology
  • Animals
  • Capsaicin / analogs & derivatives*
  • Capsaicin / chemical synthesis
  • Capsaicin / chemistry
  • Capsaicin / pharmacology
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Pain / prevention & control
  • Receptors, Drug / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Receptors, Drug
  • Capsaicin