Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Discovery of potent transient receptor potential vanilloid 1 antagonists: design and synthesis of phenoxyacetamide derivatives.

Authors: Eiki Takahashi, Noriyuki Hirano, Takashi Nagahara, Satoru Yoshikawa, Shinobu Momen, Hiroshi Yokokawa, Ryoji Hayashi

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Jun 1 , 23, 3154-6

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23632270

Abstract
We aimed to discover a novel type of transient receptor potential vanilloid 1 (TRPV1) antagonist because such antagonists are possible drug candidates for treating various disorders. We modified the structure of hit compound 7 (human TRPV1 IC50=411 nM) and converted its pyrrolidino group to a (hydroxyethyl)methylamino group, which substantially improved inhibitory activity (15d; human TRPV1 IC50=33 nM). In addition, 15d ameliorated bladder overactivity in rats in vivo.