期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 11, 页码 3746-3755出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm101621u
关键词
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资金
- Fogarty (NIH) [U01TW008163]
- NIH [ES01734]
- Department of Anesthesiology, University of Utah
New compounds nobilamides A-H and related known compounds A-3302-A and A-3302-B were isolated based upon their suppression of capsaicin-induced calcium uptake in a mouse dorsal root ganglion primary cell culture assay. Two of these compounds, nobilamide B and A-3302-A, were shown to be long-acting antagonists of mouse and human TRPV1 channels, abolishing activity for >1 h after removal of drug presumably via a covalent attachment. Other derivatives also inhibited the TRPV1 channel, albeit with low potency, affording a structure-activity profile to support the proposed mechanism of action. While the activities were modest, we propose a new mechanism of action and a new site of binding for these inhibitors that may spur development of related analogues for treatment of pain.
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