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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: kaczorowski gj. Biochemistry. 2004 Aug 3;43(30):9866-76. doi: 10.1021/bi0493259. Biochemistry. 2004. PMID: 15274641
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: kaczorowski gj. 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: kaczorowski gj. 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: kaczorowski gj. 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
Block of peripheral nerve sodium channels selectively inhibits features of neuropathic pain in rats.
Brochu RM, Dick IE, Tarpley JW, McGowan E, Gunner D, Herrington J, Shao PP, Ok D, Li C, Parsons WH, Stump GL, Regan CP, Lynch JJ Jr, Lyons KA, McManus OB, Clark S, Ali Z, Kaczorowski GJ, Martin WJ, Priest BT. Brochu RM, et al. Among authors: kaczorowski gj. Mol Pharmacol. 2006 Mar;69(3):823-32. doi: 10.1124/mol.105.018127. Epub 2005 Nov 21. Mol Pharmacol. 2006. PMID: 16301337
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: kaczorowski gj. 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
181 results