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National Institute of Environmental Health Sciences

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Publication Detail

Title: Nobilamides A-H, long-acting transient receptor potential vanilloid-1 (TRPV1) antagonists from mollusk-associated bacteria.

Authors: Lin, Zhenjian; Reilly, Christopher A; Antemano, Rowena; Hughen, Ronald W; Marett, Lenny; Concepcion, Gisela P; Haygood, Margo G; Olivera, Baldomero M; Light, Alan; Schmidt, Eric W

Published In J Med Chem, (2011 Jun 09)

Abstract: 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.

PubMed ID: 21524089 Exiting the NIEHS site

MeSH Terms: No MeSH terms associated with this publication

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