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.
Jeff DeFalco  1 ,  Daniel Steiger ,  Michelle Dourado ,  Daniel Emerling ,  Matthew A J Duncton
Affiliations
  • 1. Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), South San Francisco, CA 94080, USA. [email protected]
PMID: 20965726 DOI: 10.1016/j.bmcl.2010.09.099
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.