Chemical Name: 3-Amino-5-[[2-[(2-methoxyethyl)amino]-6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2(1H)-quinoxalinone
Biological ActivityPotent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors (IC50 values are 0.6 and 0.8 nM for capsaicin (Cat. No. 0462) and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.
Tamayo et al.
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation.
Gavva et al.
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