2. Academic Validation
  3. 5-benzyloxytryptamine as an antagonist of TRPM8

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

Affiliation

  • 1 Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), South San Francisco, CA 94080, USA. jeffrey.defalco@envoytherapeutics.com
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.

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