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Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.
Shao PP, Ye F, Chakravarty PK, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL. Shao PP, et al. Among authors: haedo rj. ACS Med Chem Lett. 2013 Sep 8;4(11):1064-8. doi: 10.1021/ml4002612. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900606 Free PMC article.
A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.
Tyagarajan S, Chakravarty PK, Park M, Zhou B, Herrington JB, Ratliff K, Bugianesi RM, Williams B, Haedo RJ, Swensen AM, Warren VA, Smith M, Garcia M, Kaczorowski GJ, McManus OB, Lyons KA, Li X, Madeira M, Karanam B, Green M, Forrest MJ, Abbadie C, McGowan E, Mistry S, Jochnowitz N, Duffy JL. Tyagarajan S, et al. Among authors: haedo rj. Bioorg Med Chem Lett. 2011 Jan 15;21(2):869-73. doi: 10.1016/j.bmcl.2010.11.067. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21195616
Characterization of the substituted N-triazole oxindole TROX-1, a small-molecule, state-dependent inhibitor of Ca(V)2 calcium channels.
Swensen AM, Herrington J, Bugianesi RM, Dai G, Haedo RJ, Ratliff KS, Smith MM, Warren VA, Arneric SP, Eduljee C, Parker D, Snutch TP, Hoyt SB, London C, Duffy JL, Kaczorowski GJ, McManus OB. Swensen AM, et al. Among authors: haedo rj. Mol Pharmacol. 2012 Mar;81(3):488-97. doi: 10.1124/mol.111.075226. Epub 2011 Dec 21. Mol Pharmacol. 2012. PMID: 22188924
Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker.
Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL. Abbadie C, et al. Among authors: haedo rj. J Pharmacol Exp Ther. 2010 Aug;334(2):545-55. doi: 10.1124/jpet.110.166363. Epub 2010 May 3. J Pharmacol Exp Ther. 2010. PMID: 20439438
Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.
Shao PP, Ye F, Chakravarty PK, Varughese DJ, Herrington JB, Dai G, Bugianesi RM, Haedo RJ, Swensen AM, Warren VA, Smith MM, Garcia ML, McManus OB, Lyons KA, Li X, Green M, Jochnowitz N, McGowan E, Mistry S, Sun SY, Abbadie C, Kaczorowski GJ, Duffy JL. Shao PP, et al. Among authors: haedo rj. J Med Chem. 2012 Nov 26;55(22):9847-55. doi: 10.1021/jm301056k. Epub 2012 Nov 12. J Med Chem. 2012. PMID: 23098566
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