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Page 1
Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice.
Uebele VN, Gotter AL, Nuss CE, Kraus RL, Doran SM, Garson SL, Reiss DR, Li Y, Barrow JC, Reger TS, Yang ZQ, Ballard JE, Tang C, Metzger JM, Wang SP, Koblan KS, Renger JJ. Uebele VN, et al. Among authors: doran sm. J Clin Invest. 2009 Jun;119(6):1659-67. doi: 10.1172/JCI36954. Epub 2009 May 18. J Clin Invest. 2009. PMID: 19451696 Free PMC article.
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: doran sm. J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10. J Med Chem. 2008. PMID: 18540666
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: doran sm. J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817368
Positive allosteric interaction of structurally diverse T-type calcium channel antagonists.
Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ. Uebele VN, et al. Among authors: doran sm. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. Cell Biochem Biophys. 2009. PMID: 19582593
Pyridyl amides as potent inhibitors of T-type calcium channels.
Reger TS, Yang ZQ, Schlegel KA, Shu Y, Mattern C, Cube R, Rittle KE, McGaughey GB, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Renger JJ, Barrow JC. Reger TS, et al. Among authors: doran sm. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21316226
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ. Whitman DB, et al. Among authors: doran sm. ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069. ChemMedChem. 2009. PMID: 19418500
Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.
Schlegel KA, Yang ZQ, Reger TS, Shu Y, Cube R, Rittle KE, Bondiskey P, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Uebele VN, Renger JJ, Barrow JC. Schlegel KA, et al. Among authors: doran sm. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8. Bioorg Med Chem Lett. 2010. PMID: 20673719
Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.
Winrow CJ, Gotter AL, Cox CD, Doran SM, Tannenbaum PL, Breslin MJ, Garson SL, Fox SV, Harrell CM, Stevens J, Reiss DR, Cui D, Coleman PJ, Renger JJ. Winrow CJ, et al. Among authors: doran sm. J Neurogenet. 2011 Mar;25(1-2):52-61. doi: 10.3109/01677063.2011.566953. Epub 2011 Apr 8. J Neurogenet. 2011. PMID: 21473737
38 results