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5-benzyloxytryptamine as an antagonist of TRPM8.

Bioorganic & medicinal chemistry letters (2010-10-23)
Jeff DeFalco, Daniel Steiger, Michelle Dourado, Daniel Emerling, Matthew A J Duncton
PMID20965726
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.

MATERIALS
Product Number
Brand
Product Description
B27803
Sigma-Aldrich
5-(Benzyloxy)indole, 95%
286583
Sigma-Aldrich
5-Methoxytryptamine, 97%