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Page 1
NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.
Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ. Lelas S, et al. Among authors: bronson jj. Neuropharmacology. 2013 Oct;73:232-40. doi: 10.1016/j.neuropharm.2013.05.038. Epub 2013 Jun 12. Neuropharmacology. 2013. PMID: 23770339
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Deshpande MS, Felsenstein KM, Guss VL, Hansel SB, Johnson G, Keavy DJ, Lau WY, Mock J, Prasad CV, Polson CT, Sloan CP, Smith DW, Wallace OB, Wang HH, Williams A, Zheng M. Parker MF, et al. Among authors: bronson jj. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. doi: 10.1016/j.bmcl.2007.06.022. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17606371
Amino-caprolactam derivatives as gamma-secretase inhibitors.
Parker MF, Bronson JJ, Barten DM, Corsa JA, Du W, Felsenstein KM, Guss VL, Izzarelli D, Loo A, McElhone KE, Marcin LR, Padmanabha R, Pak R, Polson CT, Toyn JH, Varma S, Wang J, Wong V, Zheng M, Roberts SB. Parker MF, et al. Among authors: bronson jj. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5790-5. doi: 10.1016/j.bmcl.2007.08.047. Epub 2007 Aug 26. Bioorg Med Chem Lett. 2007. PMID: 17869509
The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH. Burton CR, et al. Among authors: bronson jj. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE. Hartz RA, et al. Among authors: bronson jj. J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. J Med Chem. 2009. PMID: 19552436
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE. Hartz RA, et al. Among authors: bronson jj. J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y. J Med Chem. 2009. PMID: 19552437
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ. Hartz RA, et al. Among authors: bronson jj. J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v. J Med Chem. 2009. PMID: 19954247
5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
Schmitz WD, Brenner AB, Bronson JJ, Ditta JL, Griffin CR, Li YW, Lodge NJ, Molski TF, Olson RE, Zhuo X, Macor JE. Schmitz WD, et al. Among authors: bronson jj. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3579-83. doi: 10.1016/j.bmcl.2010.04.121. Epub 2010 May 17. Bioorg Med Chem Lett. 2010. PMID: 20483614
88 results