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Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME. Scanio MJ, et al. Among authors: liu y, liu d. Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29. Bioorg Med Chem. 2010. PMID: 20965738
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Jarvis MF, Honore P, Shieh CC, Chapman M, Joshi S, Zhang XF, Kort M, Carroll W, Marron B, Atkinson R, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa JP, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner PK, Sullivan JP, Faltynek CR, Krafte DS. Jarvis MF, et al. Among authors: liu y, liu d. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8520-5. doi: 10.1073/pnas.0611364104. Epub 2007 May 2. Proc Natl Acad Sci U S A. 2007. PMID: 17483457 Free PMC article.
Block of Nav1.8 by small molecules.
Krafte DS, Chapman M, Marron B, Atkinson R, Liu Y, Ye F, Curran M, Kort M, Jarvis MF. Krafte DS, et al. Among authors: liu y. Channels (Austin). 2007 May-Jun;1(3):152-3. doi: 10.4161/chan.4760. Epub 2007 Jul 18. Channels (Austin). 2007. PMID: 18690030 Free article.
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. I. In vitro characterization.
Gopalakrishnan M, Buckner SA, Whiteaker KL, Shieh CC, Molinari EJ, Milicic I, Daza AV, Davis-Taber R, Scott VE, Sellers D, Chess-Williams R, Chapple CR, Liu Y, Liu D, Brioni JD, Sullivan JP, Williams M, Carroll WA, Coghlan MJ. Gopalakrishnan M, et al. Among authors: liu y, liu d. J Pharmacol Exp Ther. 2002 Oct;303(1):379-86. doi: 10.1124/jpet.102.034538. J Pharmacol Exp Ther. 2002. PMID: 12235274
Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112).
McComsey DF, Smith-Swintosky VL, Parker MH, Brenneman DE, Malatynska E, White HS, Klein BD, Wilcox KS, Milewski ME, Herb M, Finley MF, Liu Y, Lubin ML, Qin N, Reitz AB, Maryanoff BE. McComsey DF, et al. Among authors: liu y. J Med Chem. 2013 Nov 27;56(22):9019-30. doi: 10.1021/jm400894u. Epub 2013 Nov 11. J Med Chem. 2013. PMID: 24205976 Free PMC article.
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