1014700-32-3Relevant articles and documents
Synthesis of benzamide derivatives as TRPV1 antagonists
Shishido, Yuji,Jinno, Madoka,Ikeda, Takafumi,Ito, Fumitaka,Sudo, Masaki,Makita, Naoya,Ohta, Atsuko,Iki-Taki, Ayako,Ohmi, Takashi,Kanai, Yoshihito,Tamura, Tetsuya,Shimojo, Masato
, p. 1072 - 1078 (2008/09/18)
From hit compounds identified by high throughput screening (HTS), we have found compound 1 as a lead TRPV1 antagonist and confirmed its potential as a treatment for pain. Compound 1 has led to potent TRPV1 antagonistic benzamide derivatives ((±)-2: human IC50 = 23 nM, (±)-3: human IC50 = 14 nM in the capsaicin-induced calcium influx assay) containing indole and naphthyl moieties, obtained by elaboration of the tryptamine scaffold or via bioisosteric replacements.