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134 results
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Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME. Scanio MJ, et al. Among authors: faltynek cr. Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29. Bioorg Med Chem. 2010. PMID: 20965738
Pore dilation occurs in TRPA1 but not in TRPM8 channels.
Chen J, Kim D, Bianchi BR, Cavanaugh EJ, Faltynek CR, Kym PR, Reilly RM. Chen J, et al. Among authors: faltynek cr. Mol Pain. 2009 Jan 21;5:3. doi: 10.1186/1744-8069-5-3. Mol Pain. 2009. PMID: 19159452 Free PMC article.
Molecular determinants of species-specific activation or blockade of TRPA1 channels.
Chen J, Zhang XF, Kort ME, Huth JR, Sun C, Miesbauer LJ, Cassar SC, Neelands T, Scott VE, Moreland RB, Reilly RM, Hajduk PJ, Kym PR, Hutchins CW, Faltynek CR. Chen J, et al. Among authors: faltynek cr. J Neurosci. 2008 May 7;28(19):5063-71. doi: 10.1523/JNEUROSCI.0047-08.2008. J Neurosci. 2008. PMID: 18463259 Free PMC article.
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
Schmidt RG, Bayburt EK, Latshaw SP, Koenig JR, Daanen JF, McDonald HA, Bianchi BR, Zhong C, Joshi S, Honore P, Marsh KC, Lee CH, Faltynek CR, Gomtsyan A. Schmidt RG, et al. Among authors: faltynek cr. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1338-41. doi: 10.1016/j.bmcl.2011.01.056. Epub 2011 Jan 21. Bioorg Med Chem Lett. 2011. PMID: 21315587
Discovery of TRPV1 antagonist ABT-116.
Brown BS, Keddy R, Perner RJ, DiDomenico S, Koenig JR, Jinkerson TK, Hannick SM, McDonald HA, Bianchi BR, Honore P, Puttfarcken PS, Moreland RB, Marsh KC, Faltynek CR, Lee CH. Brown BS, et al. Among authors: faltynek cr. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3291-4. doi: 10.1016/j.bmcl.2010.04.047. Epub 2010 Apr 14. Bioorg Med Chem Lett. 2010. PMID: 20457518
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Gomtsyan A, Bayburt EK, Keddy R, Turner SC, Jinkerson TK, Didomenico S, Perner RJ, Koenig JR, Drizin I, McDonald HA, Surowy CS, Honore P, Mikusa J, Marsh KC, Wetter JM, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: faltynek cr. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. doi: 10.1016/j.bmcl.2007.04.105. Epub 2007 May 3. Bioorg Med Chem Lett. 2007. PMID: 17507218
134 results