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Page 1
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, Connolly TM, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Marino MJ, Graufelds VK, DiLella AG, Reynolds IJ, Vargas HM, Bunting PB, Woltmann RF, Magee MM, Koblan KS, Renger JJ. Yang ZQ, et al. Among authors: graufelds vk. J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817368
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Shipe WD, Barrow JC, Yang ZQ, Lindsley CW, Yang FV, Schlegel KA, Shu Y, Rittle KE, Bock MG, Hartman GD, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Uebele VN, Nuss CE, Connolly TM, Doran SM, Fox SV, Kraus RL, Marino MJ, Graufelds VK, Vargas HM, Bunting PB, Hasbun-Manning M, Evans RM, Koblan KS, Renger JJ. Shipe WD, et al. Among authors: graufelds vk. J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10. J Med Chem. 2008. PMID: 18540666
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
Ma L, Seager MA, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, Regan C, Flick R, Pascarella D, Garson S, Doran S, Kreatsoulas C, Veng L, Lindsley CW, Shipe W, Kuduk S, Sur C, Kinney G, Seabrook GR, Ray WJ. Ma L, et al. Among authors: graufelds vk. Proc Natl Acad Sci U S A. 2009 Sep 15;106(37):15950-5. doi: 10.1073/pnas.0900903106. Epub 2009 Aug 26. Proc Natl Acad Sci U S A. 2009. PMID: 19717450 Free PMC article.