A-425619

A-425619 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).¹ It is selective for TRPV1 over a panel of 83 receptors, enzymes, transporters, and ion channels at 10 µM. A-425619 inhibits increases in intracellular calcium induced by capsaicin (Item No. 92350), N-arachidonoyl dopamine (NADA; Item No. 90057), anandamide (arachidonoyl ethanolamide; Item No. 90050), or acid in HEK293 cells expressing human TRPV1 (IC₅₀s = 5, 4, 3, and 2 nM, respectively). It increases core body temperature in rats when administered at a dose of 30 mg/kg.² A-425619 increases the paw withdrawal threshold in several rodent models of inflammatory, neuropathic, osteoarthritic, and postoperative pain in a dose-dependent manner.³

WARNING This product is not for human or veterinary use.

1. El Kouhen, R., Surowy, C.S., Bianchi, B.R., et al. 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. J. Pharmacol. Exp. Ther. 314(1), 400-409 (2005).

2. Gavva, N.R., Bannon, A.W., Surapaneni, S., et al. The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J. Neurosci. 27(13), 3366-3374 (2007).

3. Honore, P., Wismer, C.T., Mikusa, J., et al. A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats. J. Pharmacol. Exp. Ther. 314(1), 410-421 (2005).