A 425619

• Supplier: Tocris Bioscience
• Catalog: 3914
• Prices: $185.00, $755.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 581809-67-8
• Chemical Name: N-5-Isoquinolinyl-N'-[[(4-(trifluoromethyl)phenyl]methyl]urea
• Formula: C18H14F3N3O
• Molecular Weight: 345.32
• Purity: >98 %
• Description: Potent TRPV1 antagonist (IC 50 = 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 pain models.

Product References

Structure-activity relationship studies on a series of novel, substituted - Structure-activity relationship studies on a series of novel, substituted

Nelson DW, Gregg RJ, Kort ME, Perez-Medrano A, Voight EA, Wang Y, Grayson G, Namovic MT, Donnelly-Roberts DL, Niforatos W, Honore P, Jarvis MF, Faltynek CR, Carroll WA. J Med Chem. 2006 Jun 15;49(12):3659-66.

Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 - Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7

Donnelly-Roberts DL, Jarvis MF. Br J Pharmacol. 2007 Jul;151(5):571-9. Epub 2007 Apr 30.

P2X7-related modulation of pathological nociception in rats. - P2X7-related modulation of pathological nociception in rats.

McGaraughty S, Chu KL, Namovic MT, Donnelly-Roberts DL, Harris RR, Zhang XF, Shieh CC, Wismer CT, Zhu CZ, Gauvin DM, Fabiyi AC, Honore P, Gregg RJ, Kort ME, Nelson DW, Carroll WA, Marsh K, Faltynek CR, Jarvis MF. Neuroscience. 2007 Jun 8;146(4):1817-28. Epub 2007 May 3.