5-benzyloxytryptamine as an antagonist of TRPM8.
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.
DeFalco
Jeff
J
Renovis, Inc. (a wholly-owned subsidiary of Evotec AG), South San Francisco, CA 94080, USA. jeffrey.defalco@envoytherapeutics.com
Steiger
Daniel
D
Dourado
Michelle
M
Emerling
Daniel
D
Duncton
Matthew A J
MA
D000818:Animals; D006801:Humans; D020128:Inhibitory Concentration 50; D008610:Menthol / Q000494:pharmacology; D012701:Serotonin / Q000031:analogs & derivatives* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D050053:TRPM Cation Channels / Q000819:agonists / Q000037:antagonists & inhibitors*; D014363:Tryptamines / Q000494:pharmacology
D050053:TRPM Cation Channels; C425966:TRPM8 protein, human; D014363:Tryptamines; D008610:Menthol; C070179:5-benzyloxytryptamine; D012701:Serotonin; C030820:tryptamine