5-benzyloxytryptamine as an antagonist of TRPM8

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7076-9. doi: 10.1016/j.bmcl.2010.09.099. Epub 2010 Sep 22.

Abstract

5-Benzyloxytryptamine 19 was found to act as an antagonist of the TRPM8 ion-channel. For example, 19 had an IC(50) of 0.34 μM when menthol was used as the stimulating agonist. Related commercially-available tryptamine derivatives showed diminished, or no antagonist activity at TRPM8. The structural similarity of 5-benzyloxytryptamine to other literature TRPM8 antagonists was noted.

MeSH terms

  • Animals
  • Humans
  • Inhibitory Concentration 50
  • Menthol / pharmacology
  • Serotonin / analogs & derivatives*
  • Serotonin / pharmacology
  • Structure-Activity Relationship
  • TRPM Cation Channels / agonists
  • TRPM Cation Channels / antagonists & inhibitors*
  • Tryptamines / pharmacology

Substances

  • TRPM Cation Channels
  • TRPM8 protein, human
  • Tryptamines
  • Menthol
  • 5-benzyloxytryptamine
  • Serotonin
  • tryptamine