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A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat.
Honore P, Donnelly-Roberts D, Namovic MT, Hsieh G, Zhu CZ, Mikusa JP, Hernandez G, Zhong C, Gauvin DM, Chandran P, Harris R, Medrano AP, Carroll W, Marsh K, Sullivan JP, Faltynek CR, Jarvis MF. Honore P, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85. doi: 10.1124/jpet.106.111559. Epub 2006 Sep 18. J Pharmacol Exp Ther. 2006. PMID: 16982702
Painful purinergic receptors.
Donnelly-Roberts D, McGaraughty S, Shieh CC, Honore P, Jarvis MF. Donnelly-Roberts D, et al. J Pharmacol Exp Ther. 2008 Feb;324(2):409-15. doi: 10.1124/jpet.106.105890. Epub 2007 Nov 27. J Pharmacol Exp Ther. 2008. PMID: 18042830 Review.
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Florjancic AS, Peddi S, Perez-Medrano A, Li B, Namovic MT, Grayson G, Donnelly-Roberts DL, Jarvis MF, Carroll WA. Florjancic AS, et al. Among authors: donnelly roberts dl. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2089-92. doi: 10.1016/j.bmcl.2008.01.095. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18272366
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Nelson DW, Sarris K, Kalvin DM, Namovic MT, Grayson G, Donnelly-Roberts DL, Harris R, Honore P, Jarvis MF, Faltynek CR, Carroll WA. Nelson DW, et al. Among authors: donnelly roberts dl. J Med Chem. 2008 May 22;51(10):3030-4. doi: 10.1021/jm701516f. Epub 2008 Apr 26. J Med Chem. 2008. PMID: 18438986
81 results