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Page 1
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE. Kort ME, et al. Among authors: chapman ml. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. doi: 10.1016/j.bmcl.2010.08.121. Epub 2010 Sep 18. Bioorg Med Chem Lett. 2010. PMID: 20855211
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS. Jarvis MF, et al. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. doi: 10.1073/pnas.0611364104. Epub 2007 May 2. Proc Natl Acad Sci U S A. 2007. PMID: 17483457 Free PMC article.
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: chapman ml. J Med Chem. 2008 Feb 14;51(3):407-16. doi: 10.1021/jm070637u. Epub 2008 Jan 5. J Med Chem. 2008. PMID: 18176998
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Thomas JB, Johnson MS, Carroll WA, Marron BE, Chapman ML, Liu D, Krambis MJ, Shieh CC, Zhang X, Hernandez G, Gauvin DM, Mikusa JP, Zhu CZ, Joshi S, Honore P, Marsh KC, Roeloffs R, Werness S, Krafte DS, Jarvis MF, Faltynek CR, Kort ME. Drizin I, et al. Among authors: chapman ml. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. doi: 10.1016/j.bmc.2008.05.003. Epub 2008 May 6. Bioorg Med Chem. 2008. PMID: 18501613
Block of Nav1.8 by small molecules.
Krafte DS, Chapman M, Marron B, Atkinson R, Liu Y, Ye F, Curran M, Kort M, Jarvis MF. Krafte DS, et al. Channels (Austin). 2007 May-Jun;1(3):152-3. doi: 10.4161/chan.4760. Epub 2007 Jul 18. Channels (Austin). 2007. PMID: 18690030 Free article.
A-887826 is a structurally novel, potent and voltage-dependent Na(v)1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats.
Zhang XF, Shieh CC, Chapman ML, Matulenko MA, Hakeem AH, Atkinson RN, Kort ME, Marron BE, Joshi S, Honore P, Faltynek CR, Krafte DS, Jarvis MF. Zhang XF, et al. Among authors: chapman ml. Neuropharmacology. 2010 Sep;59(3):201-7. doi: 10.1016/j.neuropharm.2010.05.009. Epub 2010 Jun 1. Neuropharmacology. 2010. PMID: 20566409
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: chapman ml. 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
Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels.
McCormack K, Santos S, Chapman ML, Krafte DS, Marron BE, West CW, Krambis MJ, Antonio BM, Zellmer SG, Printzenhoff D, Padilla KM, Lin Z, Wagoner PK, Swain NA, Stupple PA, de Groot M, Butt RP, Castle NA. McCormack K, et al. Among authors: chapman ml. Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32. doi: 10.1073/pnas.1220844110. Epub 2013 Jul 1. Proc Natl Acad Sci U S A. 2013. PMID: 23818614 Free PMC article.
Recent progress in sodium channel modulators for pain.
Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA. Bagal SK, et al. Among authors: chapman ml. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Epub 2014 Jun 21. Bioorg Med Chem Lett. 2014. PMID: 25060923 Free article. Review.
56 results