5-Benzyloxytryptamine as an antagonist of TRPM8

5-Benzyloxytryptamine 19 was found to be an antagonist of TRPM8. Related tryptamine derivatives showed diminished, or no activity at 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 stimul...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.7076-7079
Hauptverfasser:	DeFalco, Jeff, Steiger, Daniel, Dourado, Michelle, Emerling, Daniel, Duncton, Matthew A.J.
Format:	Artikel
Sprache:	eng
Schlagworte:	5-Benzyloxytryptamine Animals Antagonist Antineoplastic agents Biological and medical sciences General aspects Humans Icilin Inhibitory Concentration 50 Medical sciences Menthol Menthol - pharmacology Pharmacology. Drug treatments Serotonin - analogs & derivatives Serotonin - pharmacology Structure-Activity Relationship Transient receptor potential TRP TRPM Cation Channels - agonists TRPM Cation Channels - antagonists & inhibitors TRPM8 Tryptamines - pharmacology Urinary system
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	5-Benzyloxytryptamine 19 was found to be an antagonist of TRPM8. Related tryptamine derivatives showed diminished, or no activity at 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.09.099