Bioorganic & Medicinal Chemistry Letters 2010-12-01

5-benzyloxytryptamine as an antagonist of TRPM8.

Jeff DeFalco, Daniel Steiger, Michelle Dourado, Daniel Emerling, Matthew A J Duncton

Index: Bioorg. Med. Chem. Lett. 20 , 7076-9, (2010)

Full Text: HTML

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.Copyright © 2010. Published by Elsevier Ltd.