Author/Authors :
Yuji Shishido، نويسنده , , Madoka Jinno، نويسنده , , Takafumi Ikeda، نويسنده , , Fumitaka Ito، نويسنده , , Masaki Sudo، نويسنده , , Naoya Makita، نويسنده , , Atsuko Ohta، نويسنده , , Ayako Iki-Taki، نويسنده , , Takashi Ohmi، نويسنده , , Yoshihito Kanai، نويسنده , , Tetsuya Tamura، نويسنده , , Masato Shimojo، نويسنده ,
Abstract :
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.
Keywords :
trpv1 , Vanilloid , Antagonist , Bioisostere , Tetrahydrocarbazole
