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Page 1
Substituted biaryl pyrazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH. Tyagarajan S, et al. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5480-3. doi: 10.1016/j.bmcl.2010.07.080. Epub 2010 Jul 24. Bioorg Med Chem Lett. 2010. PMID: 20709545
Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.
Tyagarajan S, Chakravarty PK, Zhou B, Fisher MH, Wyvratt MJ, Lyons K, Klatt T, Li X, Kumar S, Williams B, Felix J, Priest BT, Brochu RM, Warren V, Smith M, Garcia M, Kaczorowski GJ, Martin WJ, Abbadie C, McGowan E, Jochnowitz N, Parsons WH. Tyagarajan S, et al. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5536-40. doi: 10.1016/j.bmcl.2010.07.064. Epub 2010 Jul 21. Bioorg Med Chem Lett. 2010. PMID: 20709552
Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties.
Schmalhofer WA, Bao J, McManus OB, Green B, Matyskiela M, Wunderler D, Bugianesi RM, Felix JP, Hanner M, Linde-Arias AR, Ponte CG, Velasco L, Koo G, Staruch MJ, Miao S, Parsons WH, Rupprecht K, Slaughter RS, Kaczorowski GJ, Garcia ML. Schmalhofer WA, et al. Among authors: felix jp. Biochemistry. 2002 Jun 18;41(24):7781-94. doi: 10.1021/bi025722c. Biochemistry. 2002. PMID: 12056910
A disubstituted succinamide is a potent sodium channel blocker with efficacy in a rat pain model.
Priest BT, Garcia ML, Middleton RE, Brochu RM, Clark S, Dai G, Dick IE, Felix JP, Liu CJ, Reiseter BS, Schmalhofer WA, Shao PP, Tang YS, Chou MZ, Kohler MG, Smith MM, Warren VA, Williams BS, Cohen CJ, Martin WJ, Meinke PT, Parsons WH, Wafford KA, Kaczorowski GJ. Priest BT, et al. Among authors: felix jp. Biochemistry. 2004 Aug 3;43(30):9866-76. doi: 10.1021/bi0493259. Biochemistry. 2004. PMID: 15274641
Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.
Liang J, Brochu RM, Cohen CJ, Dick IE, Felix JP, Fisher MH, Garcia ML, Kaczorowski GJ, Lyons KA, Meinke PT, Priest BT, Schmalhofer WA, Smith MM, Tarpley JW, Williams BS, Martin WJ, Parsons WH. Liang J, et al. Among authors: felix jp. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2943-7. doi: 10.1016/j.bmcl.2005.02.093. Bioorg Med Chem Lett. 2005. PMID: 15878274
A high-capacity membrane potential FRET-based assay for NaV1.8 channels.
Liu CJ, Priest BT, Bugianesi RM, Dulski PM, Felix JP, Dick IE, Brochu RM, Knaus HG, Middleton RE, Kaczorowski GJ, Slaughter RS, Garcia ML, Köhler MG. Liu CJ, et al. Among authors: felix jp. Assay Drug Dev Technol. 2006 Feb;4(1):37-48. doi: 10.1089/adt.2006.4.37. Assay Drug Dev Technol. 2006. PMID: 16506887
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
Hoyt SB, London C, Gorin D, Wyvratt MJ, Fisher MH, Abbadie C, Felix JP, Garcia ML, Li X, Lyons KA, McGowan E, MacIntyre DE, Martin WJ, Priest BT, Ritter A, Smith MM, Warren VA, Williams BS, Kaczorowski GJ, Parsons WH. Hoyt SB, et al. Among authors: felix jp. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4630-4. doi: 10.1016/j.bmcl.2007.05.076. Epub 2007 May 27. Bioorg Med Chem Lett. 2007. PMID: 17588748
Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
Hoyt SB, London C, Ok H, Gonzalez E, Duffy JL, Abbadie C, Dean B, Felix JP, Garcia ML, Jochnowitz N, Karanam BV, Li X, Lyons KA, McGowan E, Macintyre DE, Martin WJ, Priest BT, Smith MM, Tschirret-Guth R, Warren VA, Williams BS, Kaczorowski GJ, Parsons WH. Hoyt SB, et al. Among authors: felix jp. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6172-7. doi: 10.1016/j.bmcl.2007.09.032. Epub 2007 Sep 11. Bioorg Med Chem Lett. 2007. PMID: 17889534
52 results