Potent TRPV1 antagonist (IC50
= 3-9 nM). Blocks capsaicin-evoked currents in rat DRG neurons and inhibits TRPV1-activation by anandamide
(Cat. No. 1339) and N
-arachidonoyl-dopamine. Reduces pain in inflammatory, postoperative and osteoarthritic in vivo
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A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid.
El Kouhen et al.
Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats.
McGaraughty et al.