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214 results

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Page 1
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, Didomenico S, Koenig JR, Turner S, Jinkerson T, Drizin I, Hannick SM, Macri BS, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter J, Stewart KD, Oie T, Jarvis MF, Surowy CS, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: jarvis mf. J Med Chem. 2005 Feb 10;48(3):744-52. doi: 10.1021/jm0492958. J Med Chem. 2005. PMID: 15689158
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Drizin I, Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, DiDomenico S, Koenig JR, Turner SC, Jinkerson TK, Brown BS, Keddy RG, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter JM, Polakowski JS, Segreti JA, Jarvis MF, Faltynek CR, Lee CH. Drizin I, et al. Among authors: jarvis mf. Bioorg Med Chem. 2006 Jul 15;14(14):4740-9. doi: 10.1016/j.bmc.2006.03.027. Epub 2006 Apr 18. Bioorg Med Chem. 2006. PMID: 16621571
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. Among authors: jarvis mf. 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
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Carroll WA, Kalvin DM, Perez Medrano A, Florjancic AS, Wang Y, Donnelly-Roberts DL, Namovic MT, Grayson G, Honoré P, Jarvis MF. Carroll WA, et al. Among authors: jarvis mf. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4044-8. doi: 10.1016/j.bmcl.2007.04.075. Epub 2007 Apr 27. Bioorg Med Chem Lett. 2007. PMID: 17482819
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Perner RJ, DiDomenico S, Koenig JR, Gomtsyan A, Bayburt EK, Schmidt RG, Drizin I, Zheng GZ, Turner SC, Jinkerson T, Brown BS, Keddy RG, Lukin K, McDonald HA, Honore P, Mikusa J, Marsh KC, Wetter JM, George KS, Jarvis MF, Faltynek CR, Lee CH. Perner RJ, et al. Among authors: jarvis mf. J Med Chem. 2007 Jul 26;50(15):3651-60. doi: 10.1021/jm070276i. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583335
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Kort ME, Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Johnson MS, Pacofsky GJ, Thomas JB, Carroll WA, Krambis MJ, Liu D, Shieh CC, Zhang X, Hernandez G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Marsh KC, Murray BP, Liu J, Werness S, Faltynek CR, Krafte DS, Jarvis MF, Chapman ML, Marron BE. Kort ME, et al. Among authors: jarvis mf. J Med Chem. 2008 Feb 14;51(3):407-16. doi: 10.1021/jm070637u. Epub 2008 Jan 5. J Med Chem. 2008. PMID: 18176998
214 results