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Page 1
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Boyd MJ, Collier PN, Clark MP, Deng H, Kesavan S, Ronkin SM, Waal N, Wang J, Cao J, Li P, Come J, Davies I, Duffy JP, Cochran JE, Court JJ, Chandupatla K, Jackson KL, Maltais F, O'Dowd H, Boucher C, Considine T, Taylor WP, Gao H, Chakilam A, Engtrakul J, Crawford D, Doyle E, Phillips J, Kemper R, Swett R, Empfield J, Bunnage ME, Charifson PS, Magavi SS. Boyd MJ, et al. Among authors: empfield j. J Med Chem. 2021 Dec 23;64(24):17777-17794. doi: 10.1021/acs.jmedchem.1c00948. Epub 2021 Dec 6. J Med Chem. 2021. PMID: 34871500
Pyridazinoquinolinetriones as NMDA glycine-site antagonists with oral antinociceptive activity in a model of neuropathic pain.
Bare TM, Brown DG, Horchler CL, Murphy M, Urbanek RA, Alford V, Barlaam C, Dyroff MC, Empfield JB, Forst JM, Herzog KJ, Keith RA, Kirschner AS, Lee CM, Lewis J, McLaren FM, Neilson KL, Steelman GB, Trivedi S, Vacek EP, Xiao W. Bare TM, et al. Among authors: empfield jb. J Med Chem. 2007 Jun 28;50(13):3113-31. doi: 10.1021/jm060212s. Epub 2007 Jun 2. J Med Chem. 2007. PMID: 17542571
The contribution of NaV1.6 to the efficacy of voltage-gated sodium channel inhibitors in wild type and NaV1.6 gain-of-function (GOF) mouse seizure control.
Johnson JP Jr, Focken T, Karimi Tari P, Dube C, Goodchild SJ, Andrez JC, Bankar G, Burford K, Chang E, Chowdhury S, Christabel J, Dean R, de Boer G, Dehnhardt C, Gong W, Grimwood M, Hussainkhel A, Jia Q, Khakh K, Lee S, Li J, Lin S, Lindgren A, Lofstrand V, Mezeyova J, Nelkenbrecher K, Shuart NG, Sojo L, Sun S, Waldbrook M, Wesolowski S, Wilson M, Xie Z, Zenova A, Zhang W, Scott FL, Cutts AJ, Sherrington RP, Winquist R, Cohen CJ, Empfield JR. Johnson JP Jr, et al. Among authors: empfield jr. Br J Pharmacol. 2024 Oct;181(20):3993-4011. doi: 10.1111/bph.16481. Epub 2024 Jun 24. Br J Pharmacol. 2024. PMID: 38922847
Molecular Pharmacology of Selective NaV1.6 and Dual NaV1.6/NaV1.2 Channel Inhibitors that Suppress Excitatory Neuronal Activity Ex Vivo.
Goodchild SJ, Shuart NG, Williams AD, Ye W, Parrish RR, Soriano M, Thouta S, Mezeyova J, Waldbrook M, Dean R, Focken T, Ghovanloo MR, Ruben PC, Scott F, Cohen CJ, Empfield J, Johnson JP. Goodchild SJ, et al. Among authors: empfield j. ACS Chem Neurosci. 2024 Mar 20;15(6):1169-1184. doi: 10.1021/acschemneuro.3c00757. Epub 2024 Feb 15. ACS Chem Neurosci. 2024. PMID: 38359277 Free PMC article.
Epileptogenic Channelopathies Guide Design of NBI-921352, a Highly Isoform-Selective Inhibitor of NaV1.6.
Johnson JP, Cutts AJ, Empfield JR, Cohen CJ. Johnson JP, et al. Among authors: empfield jr. In: Noebels JL, Avoli M, Rogawski MA, Vezzani A, Delgado-Escueta AV, editors. Jasper's Basic Mechanisms of the Epilepsies. 5th edition. New York: Oxford University Press; 2024. Chapter 72. In: Noebels JL, Avoli M, Rogawski MA, Vezzani A, Delgado-Escueta AV, editors. Jasper's Basic Mechanisms of the Epilepsies. 5th edition. New York: Oxford University Press; 2024. Chapter 72. PMID: 39637216 Free Books & Documents. Review.
NBI-921352, a first-in-class, NaV1.6 selective, sodium channel inhibitor that prevents seizures in Scn8a gain-of-function mice, and wild-type mice and rats.
Johnson JP, Focken T, Khakh K, Tari PK, Dube C, Goodchild SJ, Andrez JC, Bankar G, Bogucki D, Burford K, Chang E, Chowdhury S, Dean R, de Boer G, Decker S, Dehnhardt C, Feng M, Gong W, Grimwood M, Hasan A, Hussainkhel A, Jia Q, Lee S, Li J, Lin S, Lindgren A, Lofstrand V, Mezeyova J, Namdari R, Nelkenbrecher K, Shuart NG, Sojo L, Sun S, Taron M, Waldbrook M, Weeratunge D, Wesolowski S, Williams A, Wilson M, Xie Z, Yoo R, Young C, Zenova A, Zhang W, Cutts AJ, Sherrington RP, Pimstone SN, Winquist R, Cohen CJ, Empfield JR. Johnson JP, et al. Among authors: empfield jr. Elife. 2022 Mar 2;11:e72468. doi: 10.7554/eLife.72468. Elife. 2022. PMID: 35234610 Free PMC article.
Identification of aryl sulfonamides as novel and potent inhibitors of NaV1.5.
Sun S, Jia Q, Zenova AY, Lin S, Hussainkhel A, Mezeyova J, Chang E, Goodchild SJ, Xie Z, Lindgren A, de Boer G, Kwan R, Khakh K, Sojo L, Bichler P, Johnson JP Jr, Empfield JR, Cohen CJ, Dehnhardt CM, Dean R. Sun S, et al. Among authors: empfield jr. Bioorg Med Chem Lett. 2021 Aug 1;45:128133. doi: 10.1016/j.bmcl.2021.128133. Epub 2021 May 24. Bioorg Med Chem Lett. 2021. PMID: 34044121
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy.
Focken T, Burford K, Grimwood ME, Zenova A, Andrez JC, Gong W, Wilson M, Taron M, Decker S, Lofstrand V, Chowdhury S, Shuart N, Lin S, Goodchild SJ, Young C, Soriano M, Tari PK, Waldbrook M, Nelkenbrecher K, Kwan R, Lindgren A, de Boer G, Lee S, Sojo L, DeVita RJ, Cohen CJ, Wesolowski SS, Johnson JP Jr, Dehnhardt CM, Empfield JR. Focken T, et al. Among authors: empfield jr. J Med Chem. 2019 Nov 14;62(21):9618-9641. doi: 10.1021/acs.jmedchem.9b01032. Epub 2019 Oct 3. J Med Chem. 2019. PMID: 31525968
Progress in Understanding and Treating SCN2A-Mediated Disorders.
Sanders SJ, Campbell AJ, Cottrell JR, Moller RS, Wagner FF, Auldridge AL, Bernier RA, Catterall WA, Chung WK, Empfield JR, George AL Jr, Hipp JF, Khwaja O, Kiskinis E, Lal D, Malhotra D, Millichap JJ, Otis TS, Petrou S, Pitt G, Schust LF, Taylor CM, Tjernagel J, Spiro JE, Bender KJ. Sanders SJ, et al. Among authors: empfield jr. Trends Neurosci. 2018 Jul;41(7):442-456. doi: 10.1016/j.tins.2018.03.011. Epub 2018 Apr 23. Trends Neurosci. 2018. PMID: 29691040 Free PMC article. Review.
19 results