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Page 1
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
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
Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.
Tyagarajan S, Chakravarty PK, Zhou B, Taylor B, Eid R, Fisher MH, Parsons WH, Wyvratt MJ, Lyons KA, 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, Weber A, Duffy JL. Tyagarajan S, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7479-82. doi: 10.1016/j.bmcl.2010.10.017. Epub 2010 Oct 14. Bioorg Med Chem Lett. 2010. PMID: 21106456
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
Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile.
Middleton RE, Sanchez M, Linde AR, Bugianesi RM, Dai G, Felix JP, Koprak SL, Staruch MJ, Bruguera M, Cox R, Ghosh A, Hwang J, Jones S, Kohler M, Slaughter RS, McManus OB, Kaczorowski GJ, Garcia ML. Middleton RE, et al. Among authors: felix jp. Biochemistry. 2003 Nov 25;42(46):13698-707. doi: 10.1021/bi035209e. Biochemistry. 2003. PMID: 14622016
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
Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.
Ok D, Li C, Abbadie C, Felix JP, Fisher MH, Garcia ML, Kaczorowski GJ, Lyons KA, Martin WJ, Priest BT, Smith MM, Williams BS, Wyvratt MJ, Parsons WH. Ok D, et al. Among authors: felix jp. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1358-61. doi: 10.1016/j.bmcl.2005.11.051. Epub 2005 Dec 5. Bioorg Med Chem Lett. 2006. PMID: 16337121
52 results