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53 results
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Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists.
Skudlarek JW, DiMarco CN, Babaoglu K, Roecker AJ, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Wuelfing WP, Garson SL, Fox SV, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Kuduk SD, Coleman PJ. Skudlarek JW, et al. Among authors: gotter al. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1364-1370. doi: 10.1016/j.bmcl.2017.02.012. Epub 2017 Feb 9. Bioorg Med Chem Lett. 2017. PMID: 28216403
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.
Stump CA, Cooke AJ, Bruno J, Cabalu TD, Gotter AL, Harell CM, Kuduk SD, McDonald TP, O'Brien J, Renger JJ, Williams PD, Winrow CJ, Coleman PJ. Stump CA, et al. Among authors: gotter al. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5809-5814. doi: 10.1016/j.bmcl.2016.10.019. Epub 2016 Oct 14. Bioorg Med Chem Lett. 2016. PMID: 27818110
Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors.
Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM. Yin J, et al. Among authors: gotter al. Nat Struct Mol Biol. 2016 Apr;23(4):293-9. doi: 10.1038/nsmb.3183. Epub 2016 Mar 7. Nat Struct Mol Biol. 2016. PMID: 26950369
Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.
Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Garson SL, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ. Kuduk SD, et al. Among authors: gotter al. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2488-92. doi: 10.1016/j.bmcl.2015.04.066. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25981685
Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.
Roecker AJ, Mercer SP, Bergman JM, Gilbert KF, Kuduk SD, Harrell CM, Garson SL, Fox SV, Gotter AL, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ. Roecker AJ, et al. Among authors: gotter al. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4992-4999. doi: 10.1016/j.bmcl.2014.12.081. Epub 2015 Jan 6. Bioorg Med Chem Lett. 2015. PMID: 25613676
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ. Raheem IT, et al. Among authors: gotter al. Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23. Bioorg Med Chem Lett. 2015. PMID: 25577040
Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.
Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ. Roecker AJ, et al. Among authors: gotter al. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90. doi: 10.1016/j.bmcl.2014.08.041. Epub 2014 Aug 26. Bioorg Med Chem Lett. 2014. PMID: 25248679
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